Sotorasib
Sotorasib is a first-in-class irreversible covalent inhibitor of the KRAS G12C mutant protein, specifically targeting the mutant cysteine-12 residue to lock KRAS in its inactive GDP-bound state, blocking oncogenic RAS signaling in KRAS G12C-mutant non-small cell lung cancer, colorectal cancer, and other solid tumors. By selectively inhibiting the KRAS G12C variant found in approximately 13% of NSCLC patients and other tumors, it suppresses downstream RAS-MAPK and PI3K-AKT signaling driving tumor proliferation. It represents a breakthrough in targeting previously undruggable KRAS oncoproteins.
Peso Molecular
560,6000 g/mol
LogP
4,00
TPSA
102,00 Ų
Regra dos 5 de Lipinski
Aprovado
Áreas Terapêuticas
Mecanismo de Ação
Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream …
Estrutura 2D
Cite this structure
Embed this structure
SMILES
C=CC(=O)N1CCN(c2nc(=O)n(-c3c(C)ccnc3C(C)C)c3nc(-c4c(O)cccc4F)c(F)cc23)[C@@H](C)C1
InChI
InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1
Molecular Formula
C30H30F2N6O3
HBD / HBA
1 / 7
Ligações Rotacionáveis
5
Átomos Pesados
41
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Perguntas frequentes
Sotorasib is a first-in-class irreversible covalent inhibitor of the KRAS G12C mutant protein, specifically targeting the mutant cysteine-12 residue to lock KRAS in its inactive GDP-bound state, blocking oncogenic RAS signaling in KRAS G12C-mutant non-small cell lung cancer, colorectal cancer, and other solid tumors. By selectively inhibiting the KRAS G12C variant found in approximately 13% of NSCLC patients and other tumors, it suppresses downstream RAS-MAPK and PI3K-AKT signaling driving tumor proliferation. It represents a breakthrough in targeting previously undruggable KRAS …
Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.
Yes, Sotorasib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL4535757. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 137278711. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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