3023465-19-9
Chemical Structure
KRAS G12C-IN-77
- CAS No.: 3023465-19-9
- Formula:C39H34F3N7O2
- Molecular Weight:689.73
InChIKey: DZASTHQXDWTEGB-OSBSJBQFSA-N
SMILES: [H]C#CC1=CC=CC2=CC=CC(C3=C(C4=C(C(N5CCN(CC5)C(/C(F)=C/C6=NC=CC=C6)=O)=NC(OC[C@@]78CCCN7C[C@@H](C8)F)=N4)C=N3)F)=C12
Biological Activity: KRAS G12C-IN-77 is an orally active and selective KRASG12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRASG12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRASG12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer[1].
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KRAS G12C-IN-77 | KRAS G12C-IN-77 is an orally active and selective KRASG12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRASG12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRASG12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer. | |||||||||||||||||||||
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