GDC-0879 is a potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well, displaying no inhibition known to other protein kinases.
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
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Accessible (Haz class 3, 4, 5 or 8), International
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].
体内研究
The pharmacokinetic parameters for GDC-0879 following oral administration at doses of 15, 25, 50, 100, and 200 mg/kg in mice are characterized by an absorption rate constant (ka) of 8.20 h^-1, an elimination rate constant (ke) of 0.59 h^-1, and an apparent volume of distribution of 6.19 L/kg[2].
体外研究
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].
GDC-0879 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
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
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