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Tirbanibulin

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Chemical Structure| 897016-82-9 同义名 : KX-01;KX2-391
CAS号 : 897016-82-9
货号 : A161457
分子式 : C26H29N3O3
纯度 : 99%+
分子量 : 431.527
MDL号 : MFCD18633218
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(92.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

4% DMSO+30% PEG 300+water 5 mg/mL

生物活性
靶点

  • Src

    Src (HuH7), GI50:13 nM

    Src (Hep 3B), GI50:26 nM
描述 KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
mouse NIH3T3 cells Function assay 3 days Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay 21852023
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.17mL

4.63mL

2.32mL
参考文献

[1]Fallah-Tafti A, Foroumadi A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem. 2011 Oct;46(10):4853-8.

[2]Lau GM, Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci. 2009 Jul;54(7):1465-74.