Synonyms: (3-((4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)phenyl)methanesulfonamide hydrochloride; 3-[[4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl]amino]benzenemethanesulfonamide hydrochloride; BAY 958 HCl; BAY958 HCl; LDC 526 HCl; LDC526 HCl
Molecular Formula: C17H16FN5O3S · HCl
Molecular Weight: 425.86
Linear Structural Formula: C17H16FN5O3S · HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: BAY-958 (LDC526) is an orally active, ATP site-targeting, potent and selective PTEFb/CDK9 inhibitor (hCDK9-CycT1 IC50 = 5-11 nM; [ATP] = 10 muM) with 52- to >2000-fold selectivity over CDK1-7 with antiproliferative activity in cancer cultures (IC50 = 0.28 muM/96h/MOLM-13, 1 muM/96h/HeLa, 0.55 muM/48h/MEC-1, 0.28 muM/48h/CCL patient PBMCs). When administered orally in mice, BAY-958 significantly suppresses MOLM-13 acute myeloid leukemia (AML) tumor growth in mice (30/40 mg/kg/day p.o.; HCl salt) and exhibits in vivo efficacy in two murine chronic lymphocytic leukemia (CLL) models (50 & 70 mg/kg/day p.o.; free base).