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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-GDC-0623
GDC-0623

Chemical Structure : GDC-0623

CAS No.: 1168091-68-6

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GDC-0623 (RG 7421, G-868 )

货号: PC-73145Not For Human Use, Lab Use Only.

GDC-0623 (RG 7421) is a potent, selective, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM).

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10 mg ￥1980 In stock
50 mg ￥4580 In stock
100 mg ￥7280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-0623 (RG 7421) is a potent, selective, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM).
GDC-0623 displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM), prevents MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E).
GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model.

物理化学性质&存储条件

分子量 456.21
分子式 C16H14FIN4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 Month
Shipping
Solubility

Chemical Name/SMILES

参考文献

1. Hatzivassiliou G, et al. Nature. 2013 Sep 12;501(7466):232-6.

2. Robarge KD, et al. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723.

3. Zaanan A, et al. J Biol Chem. 2015 Sep 25;290(39):23838-49.

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