GDC-0623 (Synonyms: RG 7421; MEK inhibitor 1) |
Catalog No.GC14247 |
GDC-0623(RG 7421)은 MEK1의 강력한 ATP 비경쟁적 억제제(Ki=0.13 nM, +ATP)이며 HCT116(KRAS(G13D), EC50=42 nM)에 대해 6배 더 약한 효능을 나타냅니다. 대 A375(BRAFV600E, EC50=7 nM).
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Cas No.: 1168091-68-6
Sample solution is provided at 25 µL, 10mM.
GDC-0623 is a potent and ATP-uncompetitive inhibitor of MEK1 with Ki value of 0.13nM [1].
GDC-0623 is an allosteric MEK inhibitor and has efficacy against both mutant BRAF and mutant KRAS. In the cell viability assays, GDC-0623 inhibits BRAF (V600E) and KRAS (G13D) with EC50 values of 7nM and 42nM, respectively in A375 cells and HCT116 cells. Besides that, GDC-0623 shows similar efficacy in the two genotypes in a panel of BRAF and KRAS-mutant cancer cell lines. GDC-0623 is found to prevent MEK phosphorylation in cells, resulting in more effective inhibition of pERK. Furthermore, it is found that GDC-0623 blocks RAF activation through the effect on MEK. It induces dimerization of MEK with both BRAF and CRAF and stabilizes the RAF–MEK complex. In addition, GDC-0623 also suppresses RAF activation via inhibiting the formation of BRAF–CRAF heterodimer and the translocation of RAF in plasma membrane [1].
References:
[1] Hatzivassiliou G, Haling J R, Chen H, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS-versus BRAF-driven cancers. Nature, 2013, 501(7466): 232-236.
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