| CAS: | 905281-76-7 | |
| 分子式: | C19H18N4O2 | |
| 分子量: | 334.37 | |
| 英文名称: |
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| 用途: | GDC-0879是一种新型有效的，选择性B-Raf抑制剂，在A375和Colo205细胞中IC50为0.13 nM，对c-Raf也有抑制作用；对其他蛋白激酶没有抑制作用。体外研究，在V600E B-Raf 突变的A375黑色素瘤和V600E B-Raf突变的Colo205结肠癌细胞系中，GDC-0879抑制MEK1磷酸化作用时IC50分别为59和29 nM。GDC-0879有效抑制Malme3M细胞的B-raf V600E 酶促作用，IC50为0.75 μM。用GDC-0879处理，EC50值<0.5的细胞都表达B-raf V600E 致癌等位基因(A375,624,SK-MEL-28,Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34,及Colo201)。[1] |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||||
| A872681 | MACKLIN | GDC-0879 | 99% | 355元/1mg; 756元/5mg; | 咨询 | ||||||||||||||||||||||||||||||
储存：-20℃ 状态：粉末 | |||||||||||||||||||||||||||||||||||
| A796277 | MACKLIN | GDC-0879 | 10mM in DMSO | 768元/1ml; | 咨询 | ||||||||||||||||||||||||||||||
储存：-20°C | |||||||||||||||||||||||||||||||||||
| SML1953 | Sigma-Aldrich | GDC-0879 | ≥98% (HPLC) | 1364.72元/5 MG; 5493.61元/25 MG; | 咨询 | ||||||||||||||||||||||||||||||
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
产品性质
安全信息
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