KRAS inhibitor-9

Research use only, not for human use.

KRAS inhibitor-9 is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS.

KRAS inhibitor-9 is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. 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

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. Cell Viability Assay Cell Line:H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines Concentration:0, 25, 50, 100 μM Incubation Time:24, 48, and 72 hoursResult:Inhibited three NSCLC cell lines in a dose- and time-dependent manner, but not in normal lung fibroblast cell line CCD-19Lu.Western Blot Analysis Cell Line:H2122, H358 and H460 cells Concentration:0, 25, 50, 100 μM Incubation Time:48 hours Result:Reduces the levels of phosphorylation of CRAF and AKT in a dose-dependent manner in H2122, H358 and H460 cells.Apoptosis Analysis Cell Line:H2122, H358, H460 cellsConcentration:0, 25, 50, 100 μM Incubation Time:24-72 hours Result:Significantly decreased in G0/G1 phase while remarkably increased in G2/M phase after 24 hours and induced a significantly increased apoptosis for 48h in NSCLC cell lines.

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DUN09716

MAPK/ERK Signaling

Ras

KRAS

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300809-71-6

292.8

C13H9ClN2S2?

>98% (HPLC)

DMSO:230 mg/mL?(785.49 mM;?Need ultrasonic)

Nc1ccc(Sc2nc3ccccc3s2)c(Cl)c1

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(-20℃)

With Ice Pack

≥ 2 years