Dasatinib (Synonyms: 达沙替尼; BMS-354825)

目录号: HY-10181 纯度: 99.88%: FAQs
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摩尔计算器

Dasatinib (BMS-354825) 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 K_i 值分别为 16 pM 和 30 pM。Dasatinib 抑制 Bcr-Abl 和 Src 的IC₅₀ 分别为 <1.0 nM 和 0.5 nM。Dasatinib 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

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Dasatinib Chemical Structure

CAS No. : 302962-49-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥968	In-stock
5 mg	￥233	In-stock
10 mg	￥350	In-stock
50 mg	￥880	In-stock
100 mg	￥1200	In-stock
200 mg	￥1650	In-stock
500 mg	￥2400	In-stock
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5 g		询价

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Customer Review

Other Forms of Dasatinib:

MCE 顾客使用本产品发表的 98 篇科研文献

: Dasatinib purchased from MCE. Usage Cited in: Nat Cell Biol. 2023 Mar;25(3):493-507. [Abstract]; Dasatinib (50 nM; 24 or 48 h) significantly decreases MED8A and D458 cell migration.

: Dasatinib purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109. [Abstract]; YSE450-R and EC109-R cells are treated with 200 nM BIBW 2992 alone or in combination with 100 nM Dasatinib for 48 h.

: Dasatinib purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753. [Abstract]; Synergistic Decrease Bcl-2 Expression by the Combination of SAHA with Dasatinib in MCF-7 Cells.

: Dasatinib purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]; Changes in Bcl-2 protein expression in MCF-7 cells after treatment with NSC 105014, Dasatinib or ZD1839 alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

: Dasatinib purchased from MCE. Usage Cited in: Kawasaki Medical Journal. 43(2)：63-78，2017.; Western blot analysis of effects of Dasatinib (10 or 100nM) on c-Src, p-SrcY416, FAK and p-FAKY861 expression levels in KTC-1 cells and band intensities for p-SrcY416.

: Dasatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44. [Abstract]; Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively^[1]. Dasatinib also induces apoptosis and autophagy.

IC₅₀ & Target^[1]

Bcr-Abl

1.0 nM (IC₅₀)

Src

0.5 nM (IC₅₀)

lck

0.4 nM (IC₅₀)

yes

0.5 nM (IC₅₀)

c-kit

5.0 nM (IC₅₀)

PDGFRβ

28 nM (IC₅₀)

p38

100 nM (IC₅₀)

Her1

180 nM (IC₅₀)

Her2

710 nM (IC₅₀)

FGFR-1

880 nM (IC₅₀)

MEK

1700 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	8.7 μM Compound: 1, Dasatinib	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	[PMID: 25815152]
A549	IC₅₀	12.66 μM Compound: 3	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: 23521020]
A549	IC₅₀	23.73 μM Compound: Dasatinib	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	8.2 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
A549	IC₅₀	8.37 μM Compound: Dasatinib	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
BaF3	GI₅₀	< 0.0003 μM Compound: Dasatinib	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	> 1 μM Compound: Dasatinib	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 26195136]
BaF3	EC₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	EC₅₀	> 10 μM Compound: Dasatinib	Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	GI₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	> 100 nM Compound: Dasatinib	Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay	[PMID: 34011155]
BaF3	EC₅₀	> 1000 nM Compound: Dasatinib	Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	IC₅₀	0.0002 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0009 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.001 μM Compound: Dasatinib	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.001 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0013 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0019 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0023 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.003 μM Compound: Dasatinib	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.003 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0032 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.004 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.005 μM Compound: Dasatinib	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0051 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.008 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.008 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.01 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.014 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.015 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.017 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.017 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.019 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.023 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.025 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.029 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.039 μM Compound: Dasatinib	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	EC₅₀	0.04 nM Compound: Dasatinib	Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	IC₅₀	0.09 μM Compound: Dasatinib	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay	[PMID: 26814890]
BaF3	IC₅₀	0.12 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.31 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.51 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.58 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.58 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.7 nM Compound: Dasatinib	Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
BaF3	IC₅₀	0.83 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.29 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.71 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.72 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.91 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.94 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1714 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	2.5 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	3 μM Compound: Dasatinib	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	3 μM Compound: Dasatinib	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	3.6 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	3.8 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	4.5 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	5.72 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	6.55 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	6589 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	GI₅₀	9.94 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BXPC-3	EC₅₀	33 nM Compound: Dasatinib	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
CAKI-2	EC₅₀	55 nM Compound: Dasatinib	Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay	[PMID: 27010810]
CHO	IC₅₀	81.1 μM Compound: dasatinib	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
DLD-1	IC₅₀	4.6 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
DU-145	GI₅₀	0.0623 μM Compound: Dasatinib	Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay	[PMID: 25076195]
DU-145	IC₅₀	0.0623 μM Compound: Dasatinib	Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining	[PMID: 23253074]
DU-145	GI₅₀	0.16 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human DU145 cells after 48 hrs by SRB assay Cytotoxicity against human DU145 cells after 48 hrs by SRB assay	[PMID: 24015327]
HCT-116	IC₅₀	2.3 μM Compound: 3	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: 23521020]
HCT-116	IC₅₀	3.58 μM Compound: Dasatinib	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	GI₅₀	3.7 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 24015327]
HCT-116	IC₅₀	5.23 μM Compound: Dasatinib	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
HCT-116	IC₅₀	5.3 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
HEK293	EC₅₀	0.47 μM Compound: Dasatinib	Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay	[PMID: 31520926]
HEK293	IC₅₀	14.3 μM Compound: 1, Dasatinib	Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay	[PMID: 25815152]
HEK293	IC₅₀	63 nM Compound: Dasatinib	Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay	[PMID: 22770610]
HEL	GI₅₀	5.3 μM Compound: Dasatinib	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
HepG2	IC₅₀	> 5 μM Compound: dasatinib	Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
HepG2	IC₅₀	7.5 μM Compound: Dasatinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
HL-60	IC₅₀	14.97 μM Compound: Dasatinib	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
HMEC	GI₅₀	1.8 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human HMEC after 72 hrs by WST1 assay Cytotoxicity against human HMEC after 72 hrs by WST1 assay	[PMID: 24015327]
Hs-578T	GI₅₀	0.03 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay	[PMID: 24015327]
JeKo-1	IC₅₀	1325 nM Compound: Dasatinib	Growth inhibition of human Jeko-1 cells incubated for 72 hrs Growth inhibition of human Jeko-1 cells incubated for 72 hrs	[PMID: 33479666]
Jurkat	IC₅₀	> 1000 nM Compound: Dasatinib	Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
K562	IC₅₀	< 1 nM Compound: 13, BMS-354825	Antiproliferative activity against human K562 cells after 72 hrs Antiproliferative activity against human K562 cells after 72 hrs	[PMID: 15615512]
K562	IC₅₀	0.00025 μM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26814890]
K562	GI₅₀	0.0004 μM Compound: BMS-354825	Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	IC₅₀	0.000638 μM Compound: 3	Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay	[PMID: 31303996]
K562	IC₅₀	0.0007 μM Compound: 3	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 23521020]
K562	IC₅₀	0.001 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
K562	IC₅₀	0.001 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 26195136]
K562	IC₅₀	0.19 nM Compound: Dasatinib	Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
K562	IC₅₀	0.2 nM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	CC₅₀	0.25 μM Compound: VI	Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay	[PMID: 27474918]
K562	IC₅₀	0.45 μM Compound: BMS-354825	Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 26451772]
K562	IC₅₀	0.9 nM Compound: Dasatinib	Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay	[PMID: 31539241]
K562	IC₅₀	0.9 nM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34217059]
K562	IC₅₀	1 nM Compound: 2, dasatinib,BMS-354825	Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay	[PMID: 17956080]
K562	IC₅₀	11.9 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
K562	IC₅₀	11.95 μM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
K562	IC₅₀	12.83 μM Compound: BMS-354825, SPRYCEL	Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay	[PMID: 22217877]
K562	GI₅₀	9.7 μM Compound: BMS-354825	Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay	[PMID: 35944901]
KM12	GI₅₀	7.44 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human KM12 cells after 48 hrs by SRB assay Cytotoxicity against human KM12 cells after 48 hrs by SRB assay	[PMID: 24015327]
KU812 cell line	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
KU812 cell line	IC₅₀	0.1 nM Compound: Dasatinib	Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
L02	IC₅₀	> 40 μM Compound: Dasatinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
Malme-3M	GI₅₀	6.61 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay	[PMID: 24015327]
Maver1	IC₅₀	1325 nM Compound: Dasatinib	Growth inhibition of human MAVER-1 cells incubated for 72 hrs Growth inhibition of human MAVER-1 cells incubated for 72 hrs	[PMID: 33479666]
MCF7	IC₅₀	1.11 μM Compound: Dasatinib	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	IC₅₀	2.57 μM Compound: 3	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: 23521020]
MCF7	IC₅₀	8.05 μM Compound: 1a	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25899332]
MCF7	GI₅₀	8.32 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 24015327]
MDA-MB-231	GI₅₀	0.02 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay	[PMID: 24015327]
MDA-MB-231	IC₅₀	0.112 μM Compound: Dasatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
MDA-MB-231	IC₅₀	0.178 μM Compound: dasatinib	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
MDA-MB-231	IC₅₀	1.12 μM Compound: 1a	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25899332]
MDA-MB-231	IC₅₀	12 nM Compound: 13, BMS-354825	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs	[PMID: 15615512]
MDA-MB-231	EC₅₀	44 nM Compound: Dasatinib	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: 27010810]
MDA-MB-435	IC₅₀	5.147 μM Compound: Dasatinib	Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
MDA-MB-435S	IC₅₀	3.9 μM Compound: 3	Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay	[PMID: 23521020]
MEG-01	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MOLM-14	GI₅₀	2.3 μM Compound: Dasatinib	Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MV4-11	GI₅₀	3.6 μM Compound: Dasatinib	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
NCI-H1975	EC₅₀	173 nM Compound: Dasatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 27010810]
NCI-H2286	IC₅₀	0.032 μM Compound: Dasatinib	Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay	[PMID: 26191369]
NCI-H2286	IC₅₀	33.3 nM Compound: Dasatinib	Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay	[PMID: 30572178]
NCI-H23	IC₅₀	2.27 μM Compound: 3	Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H460	IC₅₀	8.99 μM Compound: 3	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H661	IC₅₀	7.8 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
NHDF	IC₅₀	0.71 μM Compound: Dasatinib	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]
PC-3	EC₅₀	232 nM Compound: Dasatinib	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: 27010810]
PC-3	IC₅₀	9.4 nM Compound: 13, BMS-354825	Antiproliferative activity against human PC3 cells after 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs	[PMID: 15615512]
SW-620	GI₅₀	8.43 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human SW620 cells after 48 hrs by SRB assay Cytotoxicity against human SW620 cells after 48 hrs by SRB assay	[PMID: 24015327]
T47D	IC₅₀	0.9 μM Compound: 3	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 23521020]
U-251	GI₅₀	2.81 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human U251 cells after 48 hrs by SRB assay Cytotoxicity against human U251 cells after 48 hrs by SRB assay	[PMID: 24015327]
U-937	GI₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
U-937	IC₅₀	> 1000 nM Compound: Dasatinib	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
U-937	IC₅₀	≥ 100 nM Compound: dasatinib	Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr	[PMID: 17684099]
U-937	IC₅₀	10.23 μM Compound: Dasatinib	Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
U-937	IC₅₀	12.2 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
U-937	IC₅₀	13.63 μM Compound: BMS-354825, SPRYCEL	Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay	[PMID: 22217877]
U-937	IC₅₀	15.02 μM Compound: Dasatinib	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
WiDr	IC₅₀	52 nM Compound: 13, BMS-354825	Antiproliferative activity against human WiDr cells after 72 hrs Antiproliferative activity against human WiDr cells after 72 hrs	[PMID: 15615512]

体外研究
(In Vitro)

Dasatinib 对 Bcr-Abl、Src、Lck、Yes、c-Kit、PDGFRβ、p38、Her1、Her2、FGFR-1 和 MEK 具有显著活性，IC₅₀<1.0、0.50、分别为 0.40、0.50、5.0、28、100、180、720、880 和 1700 nM^[1]。
与 K562 慢性粒细胞白血病 (CML)、PC3 相比，Dasatinib 显示出抗增殖活性人前列腺肿瘤、MDA-MB-231 人乳腺肿瘤和 WiDr 人结肠肿瘤细胞系，IC₅₀ 分别为 <1.0 nM、9.4 nM、12 nM 和 52 nM^[1]。

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

体内研究
(In Vivo)

Dasatinib (5 mg/kg 和 50 mg/kg，qd×10d，5 on-2 off) 在慢性粒细胞白血病 (CML) 的 K562 异种移植模型中具有有效的抗肿瘤活性和高安全边际，表明肿瘤完全消退且低多剂量水平的毒性^[1]。
Dasatinib (10 mg/kg) 的药代动力学特征适合继续推进体内药效研究。Dasatinib (10 mg/kg) 在静脉注射和口服时表现出良好的半衰期 (t_1/2s)，分别为 3.3 和 3.1 小时。本研究口服生物利用度 (F_po) 为 27%^[1]。

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

Animal Model:	Nude mice bearing K562 xenografts
Dosage:	5 mg/kg and 50 mg/kg
Administration:	Oral administration on a 5 day on and 2 day off schedule.
Result:	Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.

Animal Model:	Sprague-Dawley Rats
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral and i.v.
Result:	C_max of 13.2 and 0.5 μM for i.v. and oral, respectively.

Clinical Trial

分子量

488.01

Formula

C₂₂H₂₆ClN₇O₂S

CAS 号

302962-49-8

性状

固体

颜色

White to off-white

中文名称

达沙替尼

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 : 125 mg/mL (256.14 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	2.0491 mL	10.2457 mL	20.4914 mL
5 mM	0.4098 mL	2.0491 mL	4.0983 mL
10 mM	0.2049 mL	1.0246 mL	2.0491 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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); 澄清溶液
方案二

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); 澄清溶液
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.26 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。
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.26 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 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。
方案五

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.26 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： 0.5% CMC-Na/saline water
Solubility: 50 mg/mL (102.46 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 20% SBE-β-CD in Saline
Solubility: 2 mg/mL (4.10 mM); 悬浊液; 超声助溶
方案三

请依序添加每种溶剂： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 6.67 mg/mL (13.67 mM); 悬浊液; 超声助溶

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: 99.88%

选择批次：

Data Sheet (647 KB) SDS (393 KB)

COA (191 KB) HNMR (284 KB) RP-HPLC (243 KB) LCMS (93 KB) 元素分析报告 (207 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61. [Content Brief]

Dasatinib 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	2.0491 mL	10.2457 mL	20.4914 mL	51.2285 mL
	5 mM	0.4098 mL	2.0491 mL	4.0983 mL	10.2457 mL
	10 mM	0.2049 mL	1.0246 mL	2.0491 mL	5.1228 mL
	15 mM	0.1366 mL	0.6830 mL	1.3661 mL	3.4152 mL
	20 mM	0.1025 mL	0.5123 mL	1.0246 mL	2.5614 mL
	25 mM	0.0820 mL	0.4098 mL	0.8197 mL	2.0491 mL
	30 mM	0.0683 mL	0.3415 mL	0.6830 mL	1.7076 mL
	40 mM	0.0512 mL	0.2561 mL	0.5123 mL	1.2807 mL
	50 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0246 mL
	60 mM	0.0342 mL	0.1708 mL	0.3415 mL	0.8538 mL
	80 mM	0.0256 mL	0.1281 mL	0.2561 mL	0.6404 mL
	100 mM	0.0205 mL	0.1025 mL	0.2049 mL	0.5123 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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Dasatinib (Synonyms: 达沙替尼; BMS-354825)

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Dasatinib (Synonyms: 达沙替尼; BMS-354825)

Customer Review

Other Forms of Dasatinib:

Dasatinib 相关抗体

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Dasatinib 相关产品

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