KRAS G12C inhibitor 65

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KRASG12C IN-1

CAS No. :

MCE 国际站：KRASG12C IN-1

产品活性：KRASG12C IN-1 是一种有效的 KRAS^G12C 共价抑制剂，可将 KRAS^G12C 捕获在 GDP 结合状态。KRASG12C IN-1 对 KRAS 突变型非小细胞肺癌具有有效的抗肿瘤活性。

研究领域：GPCR/G Protein

作用靶点：Ras

In Vitro: KRASG12C IN-1 (compound 20a) (72 h) shows potent and selective antiproliferative activities against KRAS^G12C NSCLC cells, with IC₅₀s of 0.5 μM against NCI-H358 cells and 1.30 μM against NCI-H23 cells, with 7- to 21-fold selectivity over KRAS^G12S and KRAS^WT cells.
KRASG12C IN-1 (0.5-8.0 μM; 6 h) decreases the phosphorylation of ERK and AKT in KRAS^G12C-mutant NCIH358 cells.

In Vivo: KRASG12C IN-1 (compound 20a) (10-15 mg/kg; i.p. every 2 d for 21 d) inhibited tumor growth in H358 xenografts by suppressing KRAS^G12C signalling.

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