Sitneprotafib

Sitneprotafib
Clinical data
Drug classSHP2 inhibitor
Identifiers
  • (5S)-1'-[5-[(2-amino-3-chloro-4-pyridinyl)sulfanyl]pyrazin-2-yl]spiro[5,7-dihydrocyclopenta[b]pyridine-6,4'-piperidine]-5-amine
CAS Number
PubChem CID
Chemical and physical data
FormulaC21H22ClN7S
Molar mass439.97 g·mol−1
3D model (JSmol)
  • C1CN(CCC12CC3=C([C@H]2N)C=CC=N3)C4=CN=C(C=N4)SC5=C(C(=NC=C5)N)Cl
  • InChI=1S/C21H22ClN7S/c22-18-15(3-7-26-20(18)24)30-17-12-27-16(11-28-17)29-8-4-21(5-9-29)10-14-13(19(21)23)2-1-6-25-14/h1-3,6-7,11-12,19H,4-5,8-10,23H2,(H2,24,26)/t19-/m1/s1
  • Key:GKGIGIUNYOFYHZ-LJQANCHMSA-N

Sitneprotafib (JAB-3312) is a drug that acts as an inhibitor of the protein tyrosine phosphatase enzyme SHP-2 (PTPN11). It has been researched for the treatment of cancer and is in clinical trials as a combination treatment with glecirasib.[1][2][3]

References

  1. ^ Wang P, Sun X, He X, Kang D, Liu X, Liu D, et al. (May 2025). "Glecirasib, a Potent and Selective Covalent KRAS G12C Inhibitor Exhibiting Synergism with Cetuximab or SHP2 Inhibitor JAB-3312". Cancer Research Communications. 5 (5): 792–803. doi:10.1158/2767-9764.CRC-25-0001. PMC 12076188. PMID 40304209.
  2. ^ Kang D, Wang Y, Lin Y, Ma WW, Morgensztern D, Leventakos K, et al. (July 2025). "JAB-3312, a Potent Allosteric SHP2 Inhibitor That Enhances the Efficacy of RTK/RAS/MAPK and PD-1 Blockade Therapies". Clinical Cancer Research. 31 (14): 3019–3032. doi:10.1158/1078-0432.CCR-24-3691. PMID 40333694.
  3. ^ Zhong J, Zhao J, Duan J, Fang J, Fei K, Li X, et al. (November 2025). "Glecirasib plus sitneprotafib in patients with KRASG12C-mutated non-small-cell lung cancer in China: an open-label, multicentre, single-arm, phase 1/2a trial". The Lancet. Respiratory Medicine. doi:10.1016/S2213-2600(25)00258-9. PMID 41325755.
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