GDC-0879

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Chemical Structure| 905281-76-7 同义名 : AR-00341677
CAS号 : 905281-76-7
货号 : A289395
分子式 : C19H18N4O2
纯度 : 99%+
分子量 : 334.37
MDL号 : MFCD16875916
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • B-Raf

    B-Raf, IC50:0.13 nM
描述 GDC-0879 is a novel, potent, and selective inhibitor of B-Raf that inhibits pERK with an IC50 of 63 nM[1]. GDC-0879 is currently under evaluation as an antitumor agent due to its strong inhibition of the Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines. Specifically, GDC-0879 has low cellular pMEK1 inhibition IC50 values of 59 nM in A375 melanoma cells and 29 nM in Colo205 colorectal carcinoma cells[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human A375 cells Proliferation assay Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50=0.5 μM 22808911
human A375 cells Function assay Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50=1 μM 22808911
human MALME3M cells Function assay Inhibition of ERK1/2 phosphorylation in human MALME3M cells, IC50=0.063 μM 11717001
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.95mL

2.99mL

1.50mL

29.91mL

5.98mL

2.99mL
参考文献

[1]Hansen JD, et al. Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5.

[2]Wong H, et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7.