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.
分子量
560.6000 g/mol
LogP
4.00
TPSA
102.00 Ų
Lipinski 五规则
符合
治疗领域
作用机制
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 …
二维结构
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
可旋转键数
5
重原子数
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.
常见问题
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.
Embed This Widget
Add the script tag and a data attribute to embed this widget.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<div data-drugfyi="drug" data-slug="sotorasib"></div>Embed via iframe for maximum compatibility.
<iframe src="https://drugfyi.com/iframe/drug/sotorasib/" width="420" height="400" frameborder="0" style="border:0;border-radius:10px;max-width:100%" loading="lazy"></iframe>Paste this URL in WordPress, Medium, or any oEmbed-compatible platform.
https://drugfyi.com/drug/sotorasib/Add a dynamic SVG badge to your README or docs.
[](https://drugfyi.com/drug/sotorasib/)Use the native HTML custom element.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<drugfyi-drug slug="sotorasib"></drugfyi-drug>