| Bioactivity | KRAS inhibitor-9, a potent KRAS inhibitor (Kd=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[1]. | ||||||||||||
| Invitro | 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[1]. 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)[1].KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells[1].KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway[1].KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | KRAS inhibitor-9 | ||||||||||||
| CAS | 300809-71-6 | ||||||||||||
| Formula | C13H9ClN2S2 | ||||||||||||
| Molar Mass | 292.81 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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KRAS inhibitor-9
CAS: 300809-71-6 F: C13H9ClN2S2 W: 292.81
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRA
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