M4K2234

M4K2234 is an inhibitor of activin receptor-like kinase 1 (ALK1) and ALK2 (IC50s = 7 and 14 nM, respectively). M4K2234 is selective for ALK1 and ALK2 over ALK3, -4, -5, and -6 (IC50s = 168, 1,660, 1,950, and 88 nM, respectively), as well as 30 additional kinases at 1 µM, but does inhibit TRAF2- and NCK-interacting kinase (TNIK, IC50 = 41 nM). M4K2234 also inhibits ALK2 containing the gain-of-function mutations ALK2G328V, ALK2R206H, and ALK2R258G (IC50s = 3, 6, and 6 nM, respectively). It reduces BMP7-induced increases in the phosphorylation of SMAD1/5/8 in vitro when used at concentrations ranging from 100 to 10,000 nM and reduces the growth of SU-DIPG-XXI and HSJD-DIPG-007 cells derived from patients with diffuse intrinsic pontine gliomas (DIPGs) and containing the respective mutations ALK2G328W and ALK2R206H (GI50s = 0.04 and 4.3 µM, respectively). See the Structural Genomics Consortium (SGC) website for more information.Formal Name: 2-fluoro-6-methoxy-4-[4-methyl-5-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]-3-pyridinyl]-benzamide. CAS Number: 2421141-51-5. Molecular Formula: C27H31FN4O2. Formula Weight: 462.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, DMSO: Sparingly Soluble: 1-10 mg/ml, Methanol: Slightly Soluble: 0.1-1 mg/ml. SMILES: O=C(C1=C(C=C(C2=CN=CC(C3=CC=C(N4CCN(C(C)C)CC4)C=C3)=C2C)C=C1OC)F)N. InChi Code: InChI=1S/C27H31FN4O2/c1-17(2)31-9-11-32(12-10-31)21-7-5-19(6-8-21)22-15-30-16-23(18(22)3)20-13-24(28)26(27(29)33)25(14-20)34-4/h5-8,13-17H,9-12H2,1-4H3,(H2,29,33). InChi Key: RIWTUJFFSTVYPW-UHFFFAOYSA-N.