GDC-0879

产品名称：

905281-76-7
GDC-0879
2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
GDC0879
2-[4-[(1E)-1-(Hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol
1H-Inden-1-one, 2,3-dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-, oxime
5-(1-(2-Hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime
AR00341677

产品介绍：

产品说明

生化/生理作用

GDC-0879 (AR00341677) is an orally active, ATP site-targeting, highly potent Raf inhibitor (IC50 against V600E B-Raf-catalyzed MEK phophorylation = 0.13 nM with 4 μM ATP; IC50 against pERK in V600E B-Raf-expressing cells = 29 nM/Colo205, 59 nM/A375, 63 nM/Malme-3M) with great selectivity over >200 protein kinases (IC50 >1 μM). Oral administration is shown to effectively suppress Colo205 and A375 xenografts-derived tumor growth and pMEK1 in mice in vivo (35 mg/kg bid; 50-200 mg/kg qd or bid). Paradoxically, GDC-0879 also induces wild-type and enhances V600E B-Raf dimerization in an allosteric manner independent of kinase activity inhibition, resulting in selective anti-proliferation activity against V600E B-Raf cancer cells, but not in KRAS mutant or RAS/WT Raf cells, where GDC-0879 induces formation of B–C and A–B heterodimers and downstream signaling activation.

基本信息

经验(实验)分子式	C₁₉H₁₈N₄O₂
分子量	334.37
MDL编号	MFCD16875916

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear (warmed)
储存温度	2-8℃
SMILES string	OCCN(N=C1C2=CC=NC=C2)C=C1C3=CC=C4C(CC/C4=N\O)=C3

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable