Methotrexate (Synonyms: 甲氨蝶呤; Amethopterin; CL14377; WR19039)

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Methotrexate (Amethopterin) 是一种抗代谢 (antimetabolite) 和抗叶酸剂 (antifolate)，可抑制二氢叶酸还原酶，从而防止叶酸转化为四氢叶酸并抑制 DNA 合成。Methotrexate也是一种免疫抑制剂和抗肿瘤剂，用于类风湿关节炎和研究多种癌症 (如急性淋巴细胞白血病)。

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Methotrexate Chemical Structure

CAS No. : 59-05-2

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10 mM * 1 mL in DMSO	￥660	In-stock
100 mg	￥600	In-stock
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生物活性
实验参考方法
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参考文献

生物活性

Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)^[1]^[2]^[3].

IC₅₀ & Target

Traditional Cytotoxic Agents

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
5637	IC₅₀	0.016 μM Compound: Methotrexate	Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
A-427	IC₅₀	5.52 μM Compound: Methotrexate	Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
A549	IC₅₀	0.013 μM Compound: MTX	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
A549	IC₅₀	0.0135 μM Compound: MTX	Antiproliferative activity against human A549 cells after 48 hrs by MTS assay Antiproliferative activity against human A549 cells after 48 hrs by MTS assay	[PMID: 28152430]
A549	GI₅₀	0.014 μM Compound: MTX	Antiproliferative activity against human A549 cells after 48 hrs by MTS assay Antiproliferative activity against human A549 cells after 48 hrs by MTS assay	[PMID: 28711701]
A549	IC₅₀	0.014 μM Compound: MTX	Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTS assay	[PMID: 32058237]
A549	IC₅₀	0.02 μM Compound: 1a, MTX	Antiproliferative activity against A549 cells after 72 hrs in folate depleted media Antiproliferative activity against A549 cells after 72 hrs in folate depleted media	[PMID: 17127067]
A549	IC₅₀	0.1 μM Compound: 1a, MTX	Antiproliferative activity against A549 cells after 72 hrs by MTT assay Antiproliferative activity against A549 cells after 72 hrs by MTT assay	[PMID: 17127067]
A549	IC₅₀	0.25 μM Compound: MTX	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 27886545]
A549	IC₅₀	0.99 μM Compound: MTX	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human A549 cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
A549	IC₅₀	37.4 nM Compound: 1, MTX	Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion method Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion method	[PMID: 20036565]
A549	IC₅₀	39.33 μg/mL Compound: MTX	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 30554970]
A549	IC₅₀	5 nM Compound: MTX	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 20580561]
A549	IC₅₀	990 nM Compound: MTX	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
Bel-7402	IC₅₀	82.3 μM Compound: MTX	Cytotoxicity against human Bel7402 cells after 48 hrs Cytotoxicity against human Bel7402 cells after 48 hrs	[PMID: 18555562]
BGC-823	IC₅₀	0.11 μM Compound: MTX	Cytotoxicity against human BGC823 cells after 48 hrs Cytotoxicity against human BGC823 cells after 48 hrs	[PMID: 18555562]
Caco-2	IC₅₀	0.32 μg/mL Compound: Methotrexate	Cytotoxicity against human Caco2 cells after 48 hrs by MTT assay Cytotoxicity against human Caco2 cells after 48 hrs by MTT assay	10.1007/s00044-013-0773-3
Caco-2	IC₅₀	0.32 μg/mL Compound: Methotrexate	Cytotoxicity against human Caco-2 cells after 48 hrs by MTT assay Cytotoxicity against human Caco-2 cells after 48 hrs by MTT assay	[PMID: 20846760]
Caco-2	EC₅₀	1.1 μM Compound: Methotrexate	Cytotoxicity against human Caco-2 cells assessed as cell viability by XTT assay Cytotoxicity against human Caco-2 cells assessed as cell viability by XTT assay	[PMID: 20674353]
CAKI-1	IC₅₀	> 60 μg/mL Compound: methotrexate	Growth inhibition of human CAKI1 cells after 72 hrs Growth inhibition of human CAKI1 cells after 72 hrs	[PMID: 17569517]
CAKI-1	IC₅₀	25 μg/mL Compound: MTX	Inhibition of colony formation of Caki-1 cells by MTX Inhibition of colony formation of Caki-1 cells by MTX	[PMID: 2810330]
CAKI-1	IC₅₀	3 μg/mL Compound: MTX	Inhibition of colony formation of Caki-1 cells by hydrazone-linked conjugate (regiospecific coupling) of MTX and Dal K-20 Inhibition of colony formation of Caki-1 cells by hydrazone-linked conjugate (regiospecific coupling) of MTX and Dal K-20	[PMID: 2810330]
CAKI-1	IC₅₀	3.3 μg/mL Compound: MTX	Inhibition of colony formation of Caki-1 cells by amide-linked conjugate (regiospecific coupling) of MTX and Dal K-20 Inhibition of colony formation of Caki-1 cells by amide-linked conjugate (regiospecific coupling) of MTX and Dal K-20	[PMID: 2810330]
CAKI-1	IC₅₀	3.4 μg/mL Compound: MTX	Inhibition of colony formation of Caki-1 cells by hydrazone-linked conjugate of MTX and Dal K-20 Inhibition of colony formation of Caki-1 cells by hydrazone-linked conjugate of MTX and Dal K-20	[PMID: 2810330]
CAKI-1	IC₅₀	4.5 μg/mL Compound: MTX	Inhibition of colony formation of Caki-1 cells by amide-linked conjugate of MTX and Dal K-20 Inhibition of colony formation of Caki-1 cells by amide-linked conjugate of MTX and Dal K-20	[PMID: 2810330]
Cancer cell lines	IC₅₀	2.2 μM Compound: Methotrexate	Anticancer activity against Homo sapiens (human) NCI lung cancer cell assessed as inhibition of cell proliferation after 24 hr by MTT assay Anticancer activity against Homo sapiens (human) NCI lung cancer cell assessed as inhibition of cell proliferation after 24 hr by MTT assay	10.1007/s00044-012-0260-2
Cancer cell lines	IC₅₀	2.4 μM Compound: Methotrexate	Anticancer activity against human NCI lung cancer cell by MTT assay Anticancer activity against human NCI lung cancer cell by MTT assay	[PMID: 27112448]
CCRF-CEM	IC₅₀	0.004 μg/mL Compound: MTX	Compound was tested for cytotoxic activity in CCRF-CEM Human Leukemia cells by in vitro cytotoxicity assay Compound was tested for cytotoxic activity in CCRF-CEM Human Leukemia cells by in vitro cytotoxicity assay	[PMID: 11428931]
CCRF-CEM	IC₅₀	0.025 μM Compound: MTX	In vitro cytotoxicity by its growth inhibitory activity against human leukemic lymphoblasts (CEM cells). In vitro cytotoxicity by its growth inhibitory activity against human leukemic lymphoblasts (CEM cells).	[PMID: 6585550]
CCRF-CEM	EC₅₀	12 nM Compound: MTX	Concentration required to decrease cell growth by 50% in CCRF-CEM human leukemia cell line Concentration required to decrease cell growth by 50% in CCRF-CEM human leukemia cell line	[PMID: 12408727]
CCRF-CEM	EC₅₀	14.5 nM Compound: MTX	Growth inhibition of methotrexate-resistant human CCRF-CEM R30dm cells expressing low levels of folyl-poly-glutamate synthetase after 120 hrs Growth inhibition of methotrexate-resistant human CCRF-CEM R30dm cells expressing low levels of folyl-poly-glutamate synthetase after 120 hrs	[PMID: 16279780]
CCRF-CEM	IC₅₀	14.5 μM Compound: MTX	Inhibitory activity against uptake of [3H]-MTX at Folyl-polyglutamate synthase by human leukemia cells (CCRF-CEM) Inhibitory activity against uptake of [3H]-MTX at Folyl-polyglutamate synthase by human leukemia cells (CCRF-CEM)	[PMID: 8568828]
CCRF-CEM	EC₅₀	1500 nM Compound: MTX	Growth inhibition of methotrexate-transport-resistant human CCRF-CEM R2 cells after 120 hrs Growth inhibition of methotrexate-transport-resistant human CCRF-CEM R2 cells after 120 hrs	[PMID: 16279780]
CCRF-CEM	EC₅₀	1500 nM Compound: MTX	Growth inhibition of methotrexate-transport-resistant human CCRF-CEM R2 cells after 120 hrs Growth inhibition of methotrexate-transport-resistant human CCRF-CEM R2 cells after 120 hrs	[PMID: 15615538]
CCRF-CEM	EC₅₀	16 nM Compound: MTX	Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R30dm) Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R30dm)	[PMID: 12408727]
CCRF-CEM	EC₅₀	1700 nM Compound: MTX	Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R2) Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R2)	[PMID: 12408727]
CCRF-CEM	EC₅₀	595 nM Compound: MTX	Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R1) Concentration required to decrease cell growth by 50% in methotrexate-resistant CCRF-CEM human leukemia subline (R1)	[PMID: 12408727]
CCRF-CEM	EC₅₀	615 nM Compound: MTX	Growth inhibition of methotrexate-resistant human CCRF-CEM R1 cells overproducing DHFR after 120 hrs Growth inhibition of methotrexate-resistant human CCRF-CEM R1 cells overproducing DHFR after 120 hrs	[PMID: 16279780]
CCRF-CEM	EC₅₀	660 nM Compound: MTX	Growth inhibition of methotrexate-resistant human CCRF-CEM R1 cells overproducing DHFR after 120 hrs Growth inhibition of methotrexate-resistant human CCRF-CEM R1 cells overproducing DHFR after 120 hrs	[PMID: 15615538]
CCRF-CEM	EC₅₀	7.9 nM Compound: MTX	Growth inhibition of methotrexate-resistant human CCRF-CEM R30dm cells expressing low levels of folyl-poly-glutamate synthetase after 120 hrs Growth inhibition of methotrexate-resistant human CCRF-CEM R30dm cells expressing low levels of folyl-poly-glutamate synthetase after 120 hrs	[PMID: 15615538]
COLO 205	IC₅₀	3.27 μM Compound: 6	Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay	[PMID: 23968824]
COLO 320DM	IC₅₀	5.25 μM Compound: 6	Cytotoxicity against human COLO320DM cells after 48 hrs by MTT assay Cytotoxicity against human COLO320DM cells after 48 hrs by MTT assay	[PMID: 23968824]
DAN-G	IC₅₀	0.077 μM Compound: Methotrexate	Cytotoxicity against human DAN-G cells after 96 hrs by crystal violet staining Cytotoxicity against human DAN-G cells after 96 hrs by crystal violet staining	[PMID: 19243173]
DLD-1	IC₅₀	> 60 μg/mL Compound: methotrexate	Growth inhibition of human DLD1 cells after 72 hrs Growth inhibition of human DLD1 cells after 72 hrs	[PMID: 17569517]
EL4	IC₅₀	5.1 μM Compound: methotrexate	Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25951057]
Fibroblast	IC₅₀	180 nM Compound: MTX, methotrexate	Cytotoxicity against mouse wild type fibroblast cells by MTT assay Cytotoxicity against mouse wild type fibroblast cells by MTT assay	[PMID: 17383876]
HBL-100	IC₅₀	0.04 μM Compound: MTX	Anticancer activity against Homo sapiens (human) HBL100 cells after 72 hr by MTT assay Anticancer activity against Homo sapiens (human) HBL100 cells after 72 hr by MTT assay	10.1007/s00044-012-0279-4
HCT-116	GI₅₀	0.015 μM Compound: MTX	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28177228]
HCT-116	GI₅₀	0.015 μM Compound: MTX	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26994844]
HCT-116	IC₅₀	0.13 μM Compound: MTX	Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay	[PMID: 29691154]
HCT-116	GI₅₀	0.13 μM Compound: MTX	Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay	[PMID: 28711701]
HCT-116	IC₅₀	0.75 μM Compound: MTX	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 27886545]
HCT-116	IC₅₀	9.25 μM Compound: MTX	Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay	[PMID: 35964425]
HEK293	IC₅₀	1.27 μM Compound: Methotrexate	Cytotoxicity against Homo sapiens (human) HEK293 cells assessed as inhibition of cell proliferation after 24 hr by MTT assay Cytotoxicity against Homo sapiens (human) HEK293 cells assessed as inhibition of cell proliferation after 24 hr by MTT assay	10.1007/s00044-012-0260-2
HEK293	IC₅₀	28.6 nM Compound: MTX	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HEK293	IC₅₀	35 nM Compound: MTX	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HeLa	IC₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay	[PMID: 29691154]
HeLa	GI₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay	[PMID: 28711701]
HeLa	IC₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay	[PMID: 28152430]
HeLa	IC₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability by MTS assay	[PMID: 32058237]
HeLa	IC₅₀	0.1 μM Compound: MTX	Cytotoxicity against human HeLa cells after 48 hrs Cytotoxicity against human HeLa cells after 48 hrs	[PMID: 18555562]
HeLa	IC₅₀	0.82 μM Compound: MTX	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability preincubated for 12 hrs followed by 4 Gy irradiation and measured after 60 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability preincubated for 12 hrs followed by 4 Gy irradiation and measured after 60 hrs by MTT assay	[PMID: 32676149]
HeLa	IC₅₀	1.5 μM Compound: MTX	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 12 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 12 hrs by MTT assay	[PMID: 32676149]
HeLa	IC₅₀	13.69 μM Compound: MTX	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 35964425]
HeLa	IC₅₀	21 nM Compound: MTX	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HeLa	IC₅₀	27.94 μM Compound: Methotrexate	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32503691]
HeLa	IC₅₀	59.3 nM Compound: MTX	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HepG2	IC₅₀	0.3 μM Compound: Methotrexate	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for overnight by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for overnight by MTT assay	[PMID: 31260892]
HepG2	IC₅₀	0.41 μM Compound: MTX	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 27886545]
HepG2	IC₅₀	0.99 μM Compound: MTX	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
HepG2	IC₅₀	15.8 μM Compound: methotrexate	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 27186821]
HepG2	IC₅₀	21.9 μM Compound: MTX	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 35964425]
HL-60	IC₅₀	0.012 μM Compound: methotrexate	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11170674]
HL-60	IC₅₀	0.0227 μM Compound: MTX	Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay	[PMID: 28152430]
HL-60	IC₅₀	0.023 μM Compound: MTX	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability by MTS assay	[PMID: 32058237]
HL-60	IC₅₀	0.025 μM Compound: MTX	Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay	[PMID: 29691154]
HL-60	GI₅₀	0.038 μM Compound: MTX	Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay Antiproliferative activity against human HL60 cells after 48 hrs by MTS assay	[PMID: 28711701]
HL-60	IC₅₀	0.21 μM Compound: MTX	Cytotoxicity against human HL60 cells after 48 hrs Cytotoxicity against human HL60 cells after 48 hrs	[PMID: 18555562]
HL-60	IC₅₀	1.09 μM Compound: MTX	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 27886545]
HL-60	IC₅₀	6.92 nM Compound: methotrxate	Antiproliferative activity against human HL60 cells after 48 hrs by trypan blue exclusion test Antiproliferative activity against human HL60 cells after 48 hrs by trypan blue exclusion test	[PMID: 17497807]
HL-60	IC₅₀	8.9 nM Compound: MTX	Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HL-60	IC₅₀	9.8 nM Compound: MTX	Cytotoxicity against human HL60 cells assessed reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HL60 cells assessed reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HSC-2	CC₅₀	> 400 μM Compound: MTX	Cytotoxicity against human HSC-2 cells incubated for 48 hrs by MTT assay Cytotoxicity against human HSC-2 cells incubated for 48 hrs by MTT assay	[PMID: 33744685]
HT-29	GI₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay	[PMID: 28711701]
HT-29	IC₅₀	> 100 μM Compound: MTX	Antiproliferative activity against human HT29 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human HT29 cells assessed as reduction in cell viability by MTS assay	[PMID: 32058237]
HT-29	IC₅₀	0.018 μM Compound: 1a	Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by HT-29 assay Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by HT-29 assay	[PMID: 3968685]
HT-29	GI₅₀	0.04 μM Compound: Methotrexate	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23831811]
HT-29	GI₅₀	0.04 μM Compound: Methotrexate	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 21115210]
HT-29	IC₅₀	0.23 μg/mL Compound: Methotrexate	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	10.1007/s00044-013-0773-3
HT-29	IC₅₀	0.23 μg/mL Compound: Methotrexate	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 20846760]
HT-29	IC₅₀	1.4 μM Compound: MTX	Cytostatic activity against human HT-29 cells after 4 days by MTT assay Cytostatic activity against human HT-29 cells after 4 days by MTT assay	[PMID: 22480495]
HT-29	IC₅₀	3.45 μM Compound: 6	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 23968824]
HT-29	IC₅₀	4400 nM Compound: Methotrexate	Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay	[PMID: 2778449]
HT-29	IC₅₀	47.82 μg/mL Compound: MTX	Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay	[PMID: 30554970]
HUVEC	IC₅₀	6.13 μM Compound: MTX	Cytotoxicity against HUVEC assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against HUVEC assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
IGROV-1	IC₅₀	21 nM Compound: MTX	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
IGROV-1	IC₅₀	22 nM Compound: MTX	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
Jurkat	GI₅₀	1.25 μM Compound: Methotrexate	Growth inhibition of human Jurkat cells after 72 hrs by MTT assay Growth inhibition of human Jurkat cells after 72 hrs by MTT assay	[PMID: 21802949]
K562	GI₅₀	0.03 μM Compound: Methotrexate	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 21115210]
KB	IC₅₀	0.01 μM Compound: MTX	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
KB	IC₅₀	0.01 μM Compound: MTX	Antiproliferative activity against human KB cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human KB cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
KB	IC₅₀	10 nM Compound: MTX	Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
KB	IC₅₀	20 nM Compound: MTX	Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	20 nM Compound: MTX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	20 nM Compound: MTX	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid	[PMID: 24111942]
KB	IC₅₀	20 nM Compound: MTX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	20 nM Compound: MTX	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
KB	IC₅₀	20.9 μM Compound: MTX	Antiproliferative activity against human KB cells after 48 hrs Antiproliferative activity against human KB cells after 48 hrs	[PMID: 23124219]
KB	IC₅₀	6 nM Compound: MTX	Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	6 nM Compound: MTX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	6 nM Compound: MTX	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
KB	IC₅₀	6 nM Compound: MTX	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
KB	IC₅₀	6 nM Compound: MTX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	8.5 nM Compound: MTX	Inhibition of colony formation of human KB cells endogenously expressing RFC/FRalpha/PCFT incubated for 14 days by methylene blue staining based clonogenicty assay Inhibition of colony formation of human KB cells endogenously expressing RFC/FRalpha/PCFT incubated for 14 days by methylene blue staining based clonogenicty assay	[PMID: 22243528]
L1210	IC₅₀	0.0046 μM Compound: 1	Ability to inhibit L1210 murine leukemia tumor cell growth in culture after 48 hr of its exposure. Ability to inhibit L1210 murine leukemia tumor cell growth in culture after 48 hr of its exposure.	[PMID: 1992118]
LCLC-103H cell line	IC₅₀	0.025 μM Compound: Methotrexate	Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining Cytotoxicity against human LCLC-103H cells after 96 hrs by crystal violet staining	[PMID: 19243173]
LNCaP	IC₅₀	0.3 μM Compound: MTX	Cytostatic activity against human LNCAP cells after 4 days by MTT assay Cytostatic activity against human LNCAP cells after 4 days by MTT assay	[PMID: 22480495]
LOX IMVI	IC₅₀	0.057 μg/mL Compound: methotrexate	Growth inhibition of human LOX IMVI cells after 72 hrs Growth inhibition of human LOX IMVI cells after 72 hrs	[PMID: 17569517]
MCF7	IC₅₀	> 22 μM Compound: MTX	Cytotoxicity against human MCF7 cells incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells incubated for 72 hrs by SRB assay	[PMID: 33479665]
MCF7	IC₅₀	0.015 μM Compound: MTX	Antineoplastic activity against human MCF7 cells incubated for 72 hrs by prestoblue reduction assay Antineoplastic activity against human MCF7 cells incubated for 72 hrs by prestoblue reduction assay	[PMID: 33479665]
MCF7	GI₅₀	0.024 μM Compound: MTX	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28177228]
MCF7	GI₅₀	0.024 μM Compound: MTX	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26994844]
MCF7	IC₅₀	0.05 μM Compound: Methotrexate	Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
MCF7	GI₅₀	0.06 μM Compound: Methotrexate	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23831811]
MCF7	GI₅₀	0.06 μM Compound: Methotrexate	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 21115210]
MCF7	IC₅₀	0.097 μM Compound: MTX	Antiproliferative activity against human MCF7 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay Antiproliferative activity against human MCF7 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay	[PMID: 28830032]
MCF7	IC₅₀	0.8 μM Compound: MTX; Methotrexate	Cytostatic activity against human MCF7 cells preincubated for 3 hrs followed by serum treatment for 72 hrs measured on day 4 by MTT assay Cytostatic activity against human MCF7 cells preincubated for 3 hrs followed by serum treatment for 72 hrs measured on day 4 by MTT assay	[PMID: 27031212]
MCF7	EC₅₀	0.9 μM Compound: Methotrexate	Cytotoxicity against human MCF7 cells assessed as cell viability by XTT assay Cytotoxicity against human MCF7 cells assessed as cell viability by XTT assay	[PMID: 20674353]
MCF7	IC₅₀	2.26 μM Compound: Methotrexate	Anticancer activity against Homo sapiens (human) MCF7 cells assessed as inhibition of cell proliferation after 24 hr by MTT assay Anticancer activity against Homo sapiens (human) MCF7 cells assessed as inhibition of cell proliferation after 24 hr by MTT assay	10.1007/s00044-012-0260-2
MCF7	IC₅₀	25.32 μM Compound: MTX	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 35964425]
MCF7	IC₅₀	27.09 μM Compound: Methotrexate	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay	[PMID: 31404864]
MCF7	IC₅₀	31.48 μg/mL Compound: MTX	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 30554970]
MCF7	IC₅₀	49.22 μM Compound: Methotrexate	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 32503691]
MDA-MB-231	IC₅₀	> 100 μM Compound: MTX; Methotrexate	Cytostatic activity against human MDA-MB-231 cells preincubated for 3 hrs followed by serum treatment for 72 hrs measured on day 4 by MTT assay Cytostatic activity against human MDA-MB-231 cells preincubated for 3 hrs followed by serum treatment for 72 hrs measured on day 4 by MTT assay	[PMID: 27031212]
MDA-MB-231	IC₅₀	0.5 μM Compound: 3; MTX	Cytotoxicity against human MDA-MB-231 cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay Cytotoxicity against human MDA-MB-231 cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay	[PMID: 26985967]
MDA-MB-231	EC₅₀	80 μM Compound: Methotrexate	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability by XTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability by XTT assay	[PMID: 20674353]
MDA-MB-231	IC₅₀	9.49 μM Compound: MTX	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27886545]
MDA-MB-468	IC₅₀	0.2 μM Compound: 3; MTX	Cytotoxicity against human MDA-MB-468 cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay Cytotoxicity against human MDA-MB-468 cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay	[PMID: 26985967]
MEF	IC₅₀	120 nM Compound: MTX, methotrexate	Cytotoxicity against FKBP deficient MEF cells by MTT assay Cytotoxicity against FKBP deficient MEF cells by MTT assay	[PMID: 17383876]
NCI-H1299	GI₅₀	0.072 μM Compound: MTX	Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay	[PMID: 28711701]
NCI-H1299	IC₅₀	0.072 μM Compound: MTX	Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay	[PMID: 28152430]
NCI-H1299	IC₅₀	0.072 μM Compound: MTX	Antiproliferative activity against human H1299 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human H1299 cells assessed as reduction in cell viability by MTS assay	[PMID: 32058237]
NCI-H226	GI₅₀	10.25 μM Compound: Methotrexate	Growth inhibition of human NCI-H226 cells after 72 hrs by MTT assay Growth inhibition of human NCI-H226 cells after 72 hrs by MTT assay	[PMID: 21802949]
NCI-H23	IC₅₀	0.29 μg/mL Compound: methotrexate	Growth inhibition of human NCI-H23 cells after 72 hrs Growth inhibition of human NCI-H23 cells after 72 hrs	[PMID: 17569517]
NIH3T3	IC₅₀	0.24 μg/mL Compound: Methotrexate	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by MTT assay	10.1007/s00044-013-0773-3
P388	IC₅₀	66 nM Compound: Methotrexate	Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay	[PMID: 2778449]
PC-3	IC₅₀	0.027 μg/mL Compound: methotrexate	Growth inhibition of human PC3 cells after 72 hrs Growth inhibition of human PC3 cells after 72 hrs	[PMID: 17569517]
PC-3	GI₅₀	0.1 μM Compound: Methotrexate	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 21115210]
PC-3	IC₅₀	1 nM Compound: MTX	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 20580561]
PC-3	IC₅₀	28.78 μM Compound: MTX	Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay	[PMID: 35964425]
PPC-1	IC₅₀	0.01 μM Compound: 1a, MTX	Antiproliferative activity against PPC1 cells after 72 hrs in folate depleted media Antiproliferative activity against PPC1 cells after 72 hrs in folate depleted media	[PMID: 17127067]
PPC-1	IC₅₀	0.1 μM Compound: 1a, MTX	Antiproliferative activity against PPC1 cells after 72 hrs by MTT assay Antiproliferative activity against PPC1 cells after 72 hrs by MTT assay	[PMID: 17127067]
R2	IC₅₀	> 1000 nM Compound: MTX	Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	114 nM Compound: MTX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
R2	IC₅₀	114 nM Compound: MTX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
R2	IC₅₀	120.5 nM Compound: MTX	Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
R2	IC₅₀	121 nM Compound: MTX	Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
R2	IC₅₀	121 nM Compound: MTX	Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
R2	IC₅₀	121 nM Compound: MTX	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	216 nM Compound: MTX	Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4/FRalpha-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4/FRalpha-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
R2	IC₅₀	216 nM Compound: MTX	Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	216 nM Compound: MTX	Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
Raji	IC₅₀	0.04 μM Compound: methotrexate	Cytotoxicity against human Raji cells after 96 hrs by MTT assay Cytotoxicity against human Raji cells after 96 hrs by MTT assay	[PMID: 18513976]
RAW264.7	IC₅₀	159.2 μM Compound: Methotrexate	Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by WST-1 assay Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by WST-1 assay	[PMID: 31260892]
RAW264.7	IC₅₀	5.02 μM Compound: Methotrexate	Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as inhibition of NO overproduction preincubated for 1 hr prior to Escherichia coli LPS stimulation followed by further incubation for 24 hrs by Griess reagent based spectrophotome Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as inhibition of NO overproduction preincubated for 1 hr prior to Escherichia coli LPS stimulation followed by further incubation for 24 hrs by Griess reagent based spectrophotome	[PMID: 31260892]
RT-4	IC₅₀	0.04 μM Compound: Methotrexate	Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining	[PMID: 19243173]
SK-OV-3	IC₅₀	0.06 μM Compound: MTX	Antiproliferative activity against human SKOV3 cells after 48 hrs Antiproliferative activity against human SKOV3 cells after 48 hrs	[PMID: 23124219]
SNB-7	IC₅₀	> 60 μg/mL Compound: methotrexate	Growth inhibition of human SNB7 cells after 72 hrs Growth inhibition of human SNB7 cells after 72 hrs	[PMID: 17569517]
SW 1116	IC₅₀	2.49 μM Compound: Methotrexate	Antitumor activity against human SW1116 cells assessed as reduction in cell viability incubated for overnight by MTT assay Antitumor activity against human SW1116 cells assessed as reduction in cell viability incubated for overnight by MTT assay	[PMID: 31260892]
SW480	IC₅₀	0.015 μM Compound: 1a	Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by SW480 assay Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by SW480 assay	[PMID: 3968685]
SW-620	IC₅₀	0.013 μM Compound: MTX	Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
SW-620	IC₅₀	0.022 μM Compound: MTX	Antiproliferative activity against human SW620 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay Antiproliferative activity against human SW620 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay	[PMID: 28830032]
SW-620	IC₅₀	13.1 nM Compound: MTX	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
T47D	IC₅₀	0.16 μg/mL Compound: Methotrexate	Cytotoxicity against human T47D cells after 48 hrs by MTT assay Cytotoxicity against human T47D cells after 48 hrs by MTT assay	10.1007/s00044-013-0773-3
T47D	IC₅₀	0.16 μg/mL Compound: Methotrexate	Cytotoxicity against human T47D cells after 48 hrs by MTT assay Cytotoxicity against human T47D cells after 48 hrs by MTT assay	[PMID: 20846760]
T47D	IC₅₀	15 μM Compound: 3; MTX	Cytotoxicity against human T47D cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay Cytotoxicity against human T47D cells expressing Y1R assessed as reduction in cell viability treated for 8 hrs followed by culturing in proliferation medium for 72 hrs by resazurin assay	[PMID: 26985967]
WiDr	IC₅₀	0.025 μM Compound: 1a	Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by WIDR assay Evaluated for the inhibition of human gastrointestinal adenocarcinoma cells in vitro by WIDR assay	[PMID: 3968685]
ZR-75-1	IC₅₀	> 60 μg/mL Compound: methotrexate	Growth inhibition of human ZR-75-1 cells after 72 hrs Growth inhibition of human ZR-75-1 cells after 72 hrs	[PMID: 17569517]

体内研究
(In Vivo)

Methotrexate（Amethopterin）降低小鼠胸腺和脾脏指数。Methotrexate 在剂量 ≥5 mg/kg时显著降低白细胞、胸腺和脾脏淋巴细胞。但治疗组加对照组与模型组之间存在显著差异（p<0.01）。葡萄籽原花青素和西伯利亚人参刺五加苷的组合明显减弱 Methotrexate 暴露对小鼠胸腺和脾脏指数的影响^[2]。
Methotrexate (MTX)（2 mg/kg；腹腔注射；每周一次，共 5 周）对弗氏完全佐剂性关节炎有效。Methotrexate（1 mg/kg；腹腔注射；每周一次，共 5 周）和姜黄素（30 mg/kg 和 100 mg/kg，每周三次，共 5 周；腹腔注射）的组合显示出显著的抗关节炎作用和对血液毒性的保护作用^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

454.44

Formula

C₂₀H₂₂N₈O₅

CAS 号

59-05-2

性状

固体

颜色

Light yellow to yellow

中文名称

甲氨蝶呤；氨甲蝶呤；氨甲叶酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (110.03 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2005 mL	11.0026 mL	22.0051 mL
5 mM	0.4401 mL	2.2005 mL	4.4010 mL
10 mM	0.2201 mL	1.1003 mL	2.2005 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); 澄清溶液
方案四

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); 澄清溶液

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.87%

选择批次：

Data Sheet (645 KB) SDS (584 KB)

COA (285 KB) HNMR (310 KB) RP-HPLC (240 KB) LCMS (92 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73. [Content Brief]

[2]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92. [Content Brief]

[3]. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine.

[4]. Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43(5):546-550. [Content Brief]

Cell Assay ^[1]	Each cell line is studied in growth inhibition experiments using 96-well microtiter plates. As antifols are schedule dependent, preliminary experiments are aimed at defining the longest duration of exposure that would allow for continuous logarithmic phase growth of cells without changing of the culture media while maintaining a linear relationship between SRB optical density and cell number. Twenty-four hours after cell plating, the cell lines are exposed to the antifol for 120 h (three replicates per experiment). To ensure that a complete sigmoidal survival-concentration curve could be observed, the following drug concentrations are studied: Methotrexate (0.002-5 μM), AMT (0.0001-1 μM), PXD (0.0003-10 μM), TLX (0.0002-0.5 μM). Experiments are repeated at least twice^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] The combination of bioactive phytochemicals is administered one week prior to the Methotrexate exposure. Treatment group I: mice are given a combination of green tea polyphenols and eleutherosides from Siberian ginseng (0.2 mL/10 g, i.g. once daily) for 15 days, and a single dose of Methotrexate (2 mg/kg, i.p. once daily) is added on the 8th day. Treatment group II: mice are given a combination of grape seed proanthocyanidins and eleutherosides from Siberian ginseng for 15 days, and Methotrexate is administered on the 8th day in a similar manner. Model group: animals received distilled water instead of bioactive phytochemicals combinations for 15 days and the same Methotrexate protocol applied to this group on the 8th day. Control group: mice are given distilled water through 15 days and physiological saline instead of Methotrexate is administered on the 8th day in a similar manner. Twelve hours after the final doses, the animals are euthanized by cervical dislocation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis. 2007;65(3):168-73. [Content Brief] [2]. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92. [Content Brief] [3]. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity in Rat Large Intestine. [4]. Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43(5):546-550. [Content Brief]

Methotrexate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2005 mL	11.0026 mL	22.0051 mL	55.0128 mL
	5 mM	0.4401 mL	2.2005 mL	4.4010 mL	11.0026 mL
	10 mM	0.2201 mL	1.1003 mL	2.2005 mL	5.5013 mL
	15 mM	0.1467 mL	0.7335 mL	1.4670 mL	3.6675 mL
	20 mM	0.1100 mL	0.5501 mL	1.1003 mL	2.7506 mL
	25 mM	0.0880 mL	0.4401 mL	0.8802 mL	2.2005 mL
	30 mM	0.0734 mL	0.3668 mL	0.7335 mL	1.8338 mL
	40 mM	0.0550 mL	0.2751 mL	0.5501 mL	1.3753 mL
	50 mM	0.0440 mL	0.2201 mL	0.4401 mL	1.1003 mL
	60 mM	0.0367 mL	0.1834 mL	0.3668 mL	0.9169 mL
	80 mM	0.0275 mL	0.1375 mL	0.2751 mL	0.6877 mL
	100 mM	0.0220 mL	0.1100 mL	0.2201 mL	0.5501 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Methotrexate (Synonyms: 甲氨蝶呤; Amethopterin; CL14377; WR19039)

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Methotrexate (Synonyms: 甲氨蝶呤; Amethopterin; CL14377; WR19039)

Customer Review

Other Forms of Methotrexate:

Methotrexate 相关抗体

MCE 顾客使用本产品发表的 41 篇科研文献

Methotrexate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 ADC Cytotoxin 亚型特异性产品:

生物活性

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参考文献

摩尔计算器

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