KRAS inhibitor-9 是有效的 KRAS 抑制剂 (K_d=92 μM)，阻止 GTP-KRAS 的形成和 KRAS 下游激活。KRAS inhibitor-9 以中等的结合亲和力与 KRAS G12D，KRAS G12C 和 KRAS Q61H 蛋白结合。KRAS inhibitor-9 导致 G2/M 细胞周期停滞并诱导凋亡 (apoptosis)。KRAS inhibitor-9 选择性抑制具有 KRAS 突变的 NSCLC 细胞的增殖，但不抑制正常肺细胞的增殖。KRAS inhibitor-9

KRAS inhibitor-9, a potent KRAS inhibitor (K d =92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

Solid

KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively.
KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours).
KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells.
KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway.
KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Xie C, et al. Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells. Front Pharmacol. 2017;8:823. Published 2017 Nov 14.

In Vitro: DMSO : 250 mg/mL (853.80 mM; Need ultrasonic)配制储备液