Dasatinib

Cat. No. 6793 4 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Highly potent pan-Src/Bcr-Abl inhibitor

别名： BMS-354825

化学名： N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide

纯度： ≥98% (HPLC)

引用文献 (4)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Dasatinib

Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (K_i values are 16 and 30 pM, respectively. Inhibits Bcr-Abl, Src, Lck, Fyn, c-kit and Yes with IC₅₀ values in the subnanomolar range. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model. Inhibits replication of SARS-CoV and MERS-CoV in vitro (EC₅₀ values are 2.1and 5.5 μM, respectively). Dasatinib also enhances CD3-targeted lentiviral vector-mediated gene transfer by 3 to 10-fold. Targets and eliminates senescent cells. Orally bioavailable.

化合物库 for Dasatinib

Dasatinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。

技术数据 for Dasatinib

分子量	488.01
公式	C₂₂H₂₆ClN₇O₂S
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	302962-49-8
PubChem ID	3062316
InChI Key	ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Smiles	CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCO)=N1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Dasatinib

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	48.8	100

制备储备液 for Dasatinib

以下数据基于产品分子量 488.01。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.05 mL	10.25 mL	20.49 mL
5 mM	0.41 mL	2.05 mL	4.1 mL
10 mM	0.2 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.2 mL	0.41 mL

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产品说明书 for Dasatinib

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Dasatinib

参考文献是支持产品生物活性的出版物。

Das et al (2006) 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide J.Med.Chem. 49 6819 PMID: 17154512

Lombardo et al (2004) 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. 47 6658 PMID: 15615512

Dyall et al (2014) Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection. Antimicrob.Agents Chemother. 58 4885 PMID: 24841273

Braun et al (2022) Dasatinib is a potent enhancer for CAR T cell generation by CD3-targeted lentiviral vectors. Mol.Ther.Methods Clin.Dev. 28 90 PMID: 36620073

If you know of a relevant reference for Dasatinib, please let us know.

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