SML2436
BAY-958 hydrochloride
≥98% (HPLC)
别名:
(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
InChI key
WKPVFIKSRZVXOX-UHFFFAOYSA-N
SMILES string
FC1=CC=C(C2=NC(NC3=CC(CS(=O)(N)=O)=CC=C3)=NC=N2)C(OC)=C1.Cl
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
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 μM) with 52- to >2000-fold selectivity over CDK1-7 with antiproliferative activity in cancer cultures (IC50 = 0.28 μM/96h/MOLM-13, 1 μM/96h/HeLa, 0.55 μM/48h/MEC-1, 0.28 μM/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).
Orally active, ATP site-targeting, potent and selective PTEFb/CDK9 inhibitor with anti-cancer efficacy in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ulrich Lücking et al.
ChemMedChem, 12(21), 1776-1793 (2017-09-30)
Selective inhibition of exclusively transcription-regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY-958, lead optimization efforts strictly focusing on kinase selectivity, physicochemical and DMPK properties finally led to the identification of the orally available
Joachim R Göthert et al.
Oncotarget, 9(41), 26353-26369 (2018-06-15)
Onset of progression even during therapy with novel drugs remains an issue in chronic lymphocytic leukemia (CLL). Thus, there is ongoing demand for novel agents. Approaches targeting cyclin-dependent kinases (CDK) have reached the clinical trial stage. CDK9 mediating RNA transcriptional
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