AZ 628

产品说明书

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Chemical Structure| 878739-06-1 同义名 : -
CAS号 : 878739-06-1
货号 : A552174
分子式 : C27H25N5O2
纯度 : 99%
分子量 : 451.52
MDL号 : MFCD17392577
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(110.74 mM)，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：
生物活性
靶点

  • B-Raf

    B-Raf (V600E), IC50:34 nM

    B-Raf, IC50:105 nM

  • C-Raf/Raf-1

    C-Raf-1, IC50:29 nM
描述 AZ 628 is a pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=363.88 μM SANGER
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=5.82 nM SANGER
A375 cells Function assay 75 mins Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins, IC50=0.015 μM 23398453
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.07mL

2.21mL

1.11mL

22.15mL

4.43mL

2.21mL
参考文献

[1]Montagut C, Sharma SV, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008 Jun 15;68(12):4853-61.

[2]Khazak V, Astsaturov I, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609. Review. Erratum in: Expert Opin Ther Targets. 2009 Sep;13(9):1135.