Formulation: A solid
Formal Name: 2-fluoro-6-methoxy-4-[4-methyl-5-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]-3-pyridinyl]-benzamide
Purity: ≥98%
Formula Markup: C27H31FN4O2
Formula Weight: 462,6
Shelf life (days): 1460
CAS Number: 2421141-51-5
Notes: M4K2234 is an inhibitor of activin receptor-like kinase 1 (ALK1) and ALK2 (IC50s = 7 and 14 nM, respectively).{68789} 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).{68789,68790} 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).{68789} See the Structural Genomics Consortium (SGC) website for more information.
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