Divarasib

Divarasib
Identifiers
  • 1-{(3S)-4-[(7M)-7-[6-amino-4-methyl-3-(trifluoromethyl)pyridin-2-yl]-6-chloro-8-fluoro-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}quinazolin-4-yl]-3-methylpiperazin-1-yl}prop-2-en-1-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC29H32ClF4N7O2
Molar mass622.07 g·mol−1
3D model (JSmol)
  • C[C@H]1CN(CCN1C2=NC(=NC3=C(C(=C(C=C32)Cl)C4=C(C(=CC(=N4)N)C)C(F)(F)F)F)OC[C@@H]5CCCN5C)C(=O)C=C
  • InChI=1S/C29H32ClF4N7O2/c1-5-21(42)40-9-10-41(16(3)13-40)27-18-12-19(30)22(26-23(29(32,33)34)15(2)11-20(35)36-26)24(31)25(18)37-28(38-27)43-14-17-7-6-8-39(17)4/h5,11-12,16-17H,1,6-10,13-14H2,2-4H3,(H2,35,36)/t16-,17-/m0/s1
  • Key:ZRBPIAWWRPFDPY-IRXDYDNUSA-N

Divarasib (GDC-6036) is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials against various types of cancer, including colorectal cancer, lung cancer and advanced solid tumors.

See also

References

  1. ↑ Ros J, Vaghi C, Baraibar I, Saoudi González N, Rodríguez-Castells M, García A, et al. (March 2024). "Targeting KRAS G12C Mutation in Colorectal Cancer, A Review: New Arrows in the Quiver". International Journal of Molecular Sciences. 25 (6): 3304. doi:10.3390/ijms25063304. PMC 10970443. PMID 38542278.
  2. ↑ Brazel D, Nagasaka M (May 2024). "Divarasib in the Evolving Landscape of KRAS G12C Inhibitors for NSCLC". Targeted Oncology. 19 (3): 297–301. doi:10.1007/s11523-024-01055-y. PMC 11111488. PMID 38739329.
  3. ↑ Tenekeci AK, Unal AA, Ceylan F, Nahit Sendur MA (2024). "An updated overview of K-RAS G12C inhibitors in advanced stage non-small cell lung cancer". Future Oncology. 20 (37): 3019–3038. doi:10.1080/14796694.2024.2407280. PMC 11572139. PMID 39360933.