CYT387

CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively). It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM). At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines. It is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms, although kinase domain mutations can confer resistance. CYT387 also blocks paclitaxel-induced JAK2 activation in ovarian cancer cells, preventing the development of a cancer stem cell-like population following chemotherapy.Formal Name: N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide. CAS Number: 1056634-68-4. Synonyms: Momelotinib. Molecular Formula: C23H22N6O2. Formula Weight: 414.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 14 mg/ml, DMSO: 16 mg/ml. lambdamax: 292 nm. SMILES: O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2. InChi Code: InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28). InChi Key: ZVHNDZWQTBEVRY-UHFFFAOYSA-N.