KRas G12C inhibitor 3 is a compound that inhibits KRas G12C.

KRAS inhibitor-3, an efficacious inhibitor of both wild-type (WT) and oncogenic KRAS mutations, exhibits high-affinity binding (K D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, and 0.74 μM for KRAS Q61H). Additionally, it impedes the interaction between KRAS and Raf, highlighting its potential as a targeted therapeutic agent in KRAS-mutant cancers.

KRAS inhibitor-18 (compound 3-10) is a potent inhibitor of KRAS G12C (IC50: 4.74 μM). KRAS inhibitor-18 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 66.4, 11.1 μM respectively. KRAS inhibitor-18 has potential for pancreatic, colorectal and lung cancer studies.

KRAS inhibitor-16 (compound 3-11) is a potent inhibitor of KRAS G12C (IC50: 0.457 μM). KRAS inhibitor-16 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 3.06, 11.1 μM respectively. KRAS inhibitor-16 has potential to be studied in pancreatic, colorectal and lung cancers.

KRAS G12C inhibitor 61 (Example 3) demonstrates potent activity by inhibiting phospho-ERK 1/2 in MIA PaCa-2 cells, reflected in an IC50 value of 9 nM. This inhibitor is applicable in the research of pancreatic, colorectal, and lung cancers [1].

KRAS inhibitor-15 (compound 3-19) is a potent inhibitor of KRAS G12C (IC50: 0.954 μM). KRAS inhibitor-15 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 2.03, >33.3 μM, respectively. KRAS inhibitor-15 has potential to be studied in pancreatic, colorectal and lung cancers.

KRAS inhibitor-17 (compound 3-9) is a potent inhibitor of KRAS G12C (IC50: 3.37 μM). KRAS inhibitor-17 exhibits p-ERK inhibition with IC50 = 9.25 μM in MIA PaCA-2 cells and >33.3 μM in A549 cells. KRAS inhibitor-17 has the potential to be studied in pancreatic, colorectal and lung cancers.