BSc5371

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BSc5371 

BSc5371 是一种有效的、不可逆的 FLT3 抑制剂,对 FLT3 突变体 FLT3(D835H),FLT3(ITD, D835V),FLT3(ITD, F691L),FLT3-ITD 和野生型 FLT3wt 的 Kd 值分别为 1.3,0.83,1.5,5.8 和 2.3 nM。BSc5371 对 FLT3 依赖性的细胞具有细胞毒性。

BSc5371

BSc5371 Chemical Structure

CAS No. : 2286419-03-0

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生物活性

BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines[1].

IC50 & Target

Kd: 1.3 nM (LT3(D835H)), 0.83 nM (LT3(ITD, D835V)), 1.5 nM (LT3(ITD, F691L)), 5.8 nM (FLT3-ITD), 2.3 nM (FLT3wt)[1]

体外研究
(In Vitro)

BSc5371 (5 μM-0.5 nM, 77 hours) exhibits inhibitory activity against FLT3-mutated (MV4-11) cells, with an IC50 of 6 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.5 nM, 2.5 nM, 5 nM, 25 nM, 50 nM, 250 nM, 500 nM and 5 μM
Incubation Time: 77 hours
Result: Exhibited inhibitory activity against MV4-11 cells, with an IC50 of 6 nM.

分子量

485.60

Formula

C24H31N5O4S

CAS 号

2286419-03-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Bensinger D, et al. Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. J Med Chem. 2019 Mar 14;62(5):2428-2446.

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