GDC-0623
Cat. No.:YN350164
CAS No. :1168091-68-6
产品名称: | GDC-0623 |
CAS No.: | 1168091-68-6 |
Chemical Name: | 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-imidazo[1,5-a]pyridine-6-carboxamide |
Synonyms: | RG 7421; MEK inhibitor 1 |
分子量: | 456.21 |
分子式: | C₁₆H₁₄FIN₄O₃ |
SMILES: | FC(C=C(I)C=C1)=C1NC2=C(C(NOCCO)=O)C=CC3=CN=CN23 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | GDC-0623 (RG 7421) 是一种有效的,ATP 竞争性的MEK1抑制剂,Ki值为 0.13 nM,对 HCT116 细胞中 KRAS (G13D)的 EC50值为 42 nM,而对 A375 细胞中 BRAFV600E的 EC50值为 7 nM。 |
IC50和靶点: | [{name:"MEK1:0.13 nM (Ki, +ATP)"}] |
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Hatzivassiliou, G., Haling, J.R., Chen, H., et al.Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancersNature501(7466),232-236(2013)
Zaanan, A., Okamoto, K., Kawakami, H., et al.The mutant KRAS gene up-regulates BCL-XL protein via STAT3 to confer apoptosis resistance that is reversed by BIM protein induction and BCL-XL antagonismJ. Biol. Chem.290(39),23838-23849(2015)