Oritinib

Oritinib is an inhibitor of mutant EGFR. It selectively inhibits EGFRL858R, EGFRL858R/T790M, EGFRDelta746-750, and EGFRDelta746-750/T790M (IC50s = 0. 0. 1. and 0. nM, respectively) over wild-type EGFR (IC50 = 18 nM). In vivo, oritinib (2. 5, and 15 mg/kg) inhibits tumor growth in PC-9 and H1975 mouse xenograft models expressing EGFRDelta746-750 and EGFRL858R/T790M, respectively. Formal Name: N-[2-[[2-(dimethylamino)ethyl]methylamino]-4- methoxy-5-[[4-(6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide. CAS Number: 2035089-28-0. Synonyms: SH-1028. Molecular Formula: C31H37N7O2. Formula Weight: 539.7. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml DMSO: Slightly Soluble: 0.1-1 mg/ml. SMILES: O=C(C=C)NC1=CC(NC2=NC(C3=C(CCCC4)N4C5=C3C=CC=C5)=CC=N2)=C(OC)C=C1N(C)CCN(C)C. InChi Code: InChI=1S/C31H37N7O2/c1-6-29(39)33-23-19-24(28(40-5)20-27(23)37(4)18-17-36(2)3)35-31-32-15-14-22(34-31)30-21-11-7-8-12-25(21)38-16-10-9-13-26(30)38/h6-8,11-12,14-15,19-20H,1,9-10,13,16-18H2,2-5H3,(H,33,39)(H,32,34,35). InChi Key: PLUKVDOZEJBBIS-UHFFFAOYSA-N. Storage: -20°C. Stability: > 4 years.