Axitinib (Synonyms: 阿昔替尼; AG-013736)

目录号: HY-10065 纯度: 99.90%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Axitinib是多靶点的酪氨酸激酶抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3， PDGFRβ 的 IC₅₀ 值分别为 0.1, 0.2, 0.1-0.3, 1.6 nM。

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Axitinib Chemical Structure

CAS No. : 319460-85-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥616	In-stock
50 mg	￥560	In-stock
100 mg	￥900	In-stock
200 mg	￥1475	In-stock
500 mg	￥2613	In-stock
1 g		询价
5 g		询价

or 大包装询价

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Customer Review

Other Forms of Axitinib:

MCE 顾客使用本产品发表的 26 篇科研文献

Cell Viability Assay

: Axitinib purchased from MCE. Usage Cited in: Sci Pharm. 2023 Feb;91(1), 12.; Axitinib (1, 10, 30 µM; 24 h) inhibits viability of MCF-7 cells.

Axitinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 VEGFR 亚型特异性产品:

查看所有亚型

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 PDGFR 亚型特异性产品:

查看所有亚型

PDGFR PDGFRβ PDGFRα

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

IC₅₀ & Target^[1]

VEGFR1

0.1 nM (IC₅₀)

VEGFR2

0.2 nM (IC₅₀)

VEGFR3

0.1 nM (IC₅₀)

PDGFRβ

1.6 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
518A2	IC₅₀	4.4 μM Compound: Axitinib	Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
A549	IC₅₀	> 25 μM Compound: Axitinib	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
A549	IC₅₀	22.4 μM Compound: Axitinib	Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay	[PMID: 30108994]
A549	IC₅₀	4.88 μM Compound: II	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
BaF3	GI₅₀	0.002 μM Compound: 6	Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.005 μM Compound: 6	Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.007 μM Compound: 6	Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.012 μM Compound: 6	Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.013 μM Compound: 6	Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.014 μM Compound: 6	Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.105 μM Compound: 6	Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.108 μM Compound: 6	Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.11 μM Compound: 8	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.12 μM Compound: 8	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.129 μM Compound: 6	Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.156 μM Compound: 6	Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.2 μM Compound: 8	Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.24 μM Compound: 8	Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.35 μM Compound: 8	Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.406 μM Compound: 6	Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.83 μM Compound: 8	Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.84 μM Compound: 8	Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.01 μM Compound: 8	Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.46 μM Compound: 8	Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.64 μM Compound: 6	Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.64 μM Compound: 8	Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.72 μM Compound: 6	Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.82 μM Compound: 6	Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.91 μM Compound: 8	Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	2.02 μM Compound: 6	Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	2.63 μM Compound: 8	Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
CHO	GI₅₀	> 10 μM Compound: 8	Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay	[PMID: 30317026]
EA.hy 926	IC₅₀	6.1 μM Compound: Axitinib	Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HCC1954	GI₅₀	2.7 μM Compound: 1	Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
HCT-116	IC₅₀	> 25 μM Compound: Axitinib	Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
HCT-116	IC₅₀	> 25 μM Compound: Axitinib	Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
HCT-116	IC₅₀	1.5 μM Compound: Axitinib	Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HCT-116	IC₅₀	1.6 μM Compound: Axitinib	Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HEK-293T	IC₅₀	46.82 μM Compound: II	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
HepG2	IC₅₀	38.7 μM Compound: Axitinib	Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay	[PMID: 30108994]
HL-60	GI₅₀	6.78 μM Compound: 8	Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
HT-29	IC₅₀	13.12 μM Compound: II	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
K562	GI₅₀	0.94 μM Compound: 8	Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
KB-V1	IC₅₀	12.9 μM Compound: Axitinib	Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
KU812 cell line	GI₅₀	0.5 μM Compound: 8	Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MCF7	IC₅₀	> 25 μM Compound: Axitinib	Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
MCF7	GI₅₀	0.97 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MCF7	GI₅₀	2.3 μM Compound: 3	Cytotoxicity against human MCF7 cells after 5 days by SRB assay Cytotoxicity against human MCF7 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-231	GI₅₀	11 μM Compound: 3	Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-231	GI₅₀	7.3 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MDA-MB-468	GI₅₀	1.3 μM Compound: 1	Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MDA-MB-468	GI₅₀	2.8 μM Compound: 3	Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay	[PMID: 24867403]
MEC1	GI₅₀	1.54 μM Compound: 8	Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MEG-01	GI₅₀	0.97 μM Compound: 8	Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
NHDF	IC₅₀	> 25 μM Compound: Axitinib	Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
OCI-AML2	GI₅₀	2.36 μM Compound: 8	Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
PC-3	IC₅₀	16.43 μM Compound: II	Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
Sf9	IC₅₀	0.0002 μM Compound: 8	Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
Sf9	IC₅₀	0.001 μM Compound: 8	Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8	[PMID: 30317026]
Sf9	IC₅₀	0.092 μM Compound: 8	Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G	[PMID: 30317026]
Sf9	IC₅₀	0.17 μM Compound: 8	Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
Sf9	IC₅₀	39 nM Compound: II	Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay	[PMID: 31445229]
SK-BR-3	GI₅₀	3.8 μM Compound: 1	Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
SK-BR-3	GI₅₀	4.6 μM Compound: 3	Cytotoxicity against human SKBR3 cells after 5 days by SRB assay Cytotoxicity against human SKBR3 cells after 5 days by SRB assay	[PMID: 24867403]
U-87MG ATCC	IC₅₀	21.7 μM Compound: II	Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
U-937	GI₅₀	1.98 μM Compound: 8	Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay	[PMID: 30317026]

体外研究
(In Vitro)

Axitinib (AG-013736) 是一种有效的选择性 VEGFR 1 至 3 抑制剂。在转染或内源性 RTK 表达细胞中，Axitinib 有效阻断生长因子刺激的 VEGFR-2 和 VEGFR-3 磷酸化，平均 IC₅₀ 值分别为 0.2 和 0.1 至 0.3 nM。基于 Axitinib 的蛋白结合，针对 VEGFR-1 的细胞活性为 1.2 nM (在存在 2.3% 牛血清白蛋白的情况下测量)，相当于绝对 IC₅₀ ~0.1 nM。在 Flk-1 转染的 NIH-3T3 细胞中针对鼠 VEGFR-2 (Flk-1) 的效力为 0.18 nM，与其人类同系物相似。Axitinib 对密切相关的 III 型和 V 型家族 RTK，包括 PDGFR-β (1.6 nM)、KIT (1.7 nM) 和 PDGFR-α，显示出约 8 至 25 倍的 IC₅₀ (5 nM)；纳摩尔浓度的 Axitinib 可阻断 PDGF BB 介导的人神经胶质瘤 U87MG 细胞 (PDGFR-β 阳性) 迁移，但不会阻断增殖^[2]。

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

体内研究
(In Vivo)

与对照肿瘤相比，单次口服剂量的 Axitinib (100 mg/kg) 显著抑制小鼠 VEGFR-2 磷酸化长达 7 小时。Axitinib 快速抑制 VEGF 诱导的小鼠皮肤血管通透性；这种抑制是剂量依赖性的，并且与小鼠体内的药物浓度直接相关。药代动力学/药效学分析表明未结合的 EC₅₀ 为 0.46 nM。在没有外源性 VEGF-A 刺激的 MV522 荷瘤小鼠的皮肤中也显示出类似的抑制作用。Axitinib 抑制小鼠人异种移植肿瘤的生长。无论初始肿瘤大小、模型类型或植入部位如何，阿西替尼都会产生剂量依赖性生长延迟^[2]。

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

Clinical Trial

分子量

386.47

Formula

C₂₂H₁₈N₄OS

CAS 号

319460-85-0

性状

固体

颜色

White to light yellow

中文名称

阿昔替尼；阿西替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 20.83 mg/mL (53.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5875 mL	12.9376 mL	25.8752 mL
5 mM	0.5175 mL	2.5875 mL	5.1750 mL
10 mM	0.2588 mL	1.2938 mL	2.5875 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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: ≥ 2.08 mg/mL (5.38 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (5.38 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.38 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 20% HP-β-CD/10 mM Citrate pH 2.0
Solubility: 8.33 mg/mL (21.55 mM); 澄清溶液; Need ultrasonic and adjust pH to 3 with H₂O

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）。

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: 99.94%

选择批次：

Data Sheet (661 KB) SDS (597 KB)

COA (291 KB) HNMR (256 KB) LCMS (187 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [Content Brief]

[2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [Content Brief]

[3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60. [Content Brief]

Cell Assay ^[2]	Endothelial or tumor cells are starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib is added and cells are incubated for 45 min at 37°C in the presence of 1 mM Na₃VO₄. The appropriate growth factor is added to the cells, and after 5 min, cells are rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates are incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes are conjugated to protein A beads and supernatants are separated by SDS-PAGE^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice and Rats^[2] Mice with M24met xenograft tumors (400-600 mm³) are administered with a single dose of Axitinib or the control (0.5% carboxymethylcellulose/H₂O). Blood and tumor tissue samples are collected for pharmacokinetic and VEGFR-2 measurements. Total protein concentrations in tumor tissues are determined using the Bradford colorimetric assay. Six-day-old Sprague-Dawley rats are given two i.p. injections of Axitinib (30 mg/kg ). Animals are sacrificed, retinas are collected and lysed, and immunoprecipitation/immunoblotting experiments are done. ECL-Plus is used for detection and densitometry analysis is done using the Alpha Imager 8800. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [Content Brief] [2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [Content Brief] [3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60. [Content Brief]

Axitinib 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	2.5875 mL	12.9376 mL	25.8752 mL	64.6881 mL
	5 mM	0.5175 mL	2.5875 mL	5.1750 mL	12.9376 mL
	10 mM	0.2588 mL	1.2938 mL	2.5875 mL	6.4688 mL
	15 mM	0.1725 mL	0.8625 mL	1.7250 mL	4.3125 mL
	20 mM	0.1294 mL	0.6469 mL	1.2938 mL	3.2344 mL
	25 mM	0.1035 mL	0.5175 mL	1.0350 mL	2.5875 mL
	30 mM	0.0863 mL	0.4313 mL	0.8625 mL	2.1563 mL
	40 mM	0.0647 mL	0.3234 mL	0.6469 mL	1.6172 mL
	50 mM	0.0518 mL	0.2588 mL	0.5175 mL	1.2938 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.

Keywords:

Axitinib319460-85-0AG-013736阿昔替尼阿西替尼AG013736AG 013736VEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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Axitinib (Synonyms: 阿昔替尼; AG-013736)

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MCE 顾客使用本产品发表的 26 篇科研文献

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Axitinib (Synonyms: 阿昔替尼; AG-013736)

Customer Review

Other Forms of Axitinib:

Axitinib 相关抗体

MCE 顾客使用本产品发表的 26 篇科研文献

Axitinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 VEGFR 亚型特异性产品:

查看 PDGFR 亚型特异性产品:

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参考文献

Axitinib 相关抗体:

摩尔计算器

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Axitinib 相关分类

完整储备液配制表

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