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BAY-958 hydrochloride
产品别名
1424871-27-1
BAY-958 hydrochloride
BAY 958 HCl
LDC 526 HCl
(3-((4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)phenyl)methanesulfonamide hydrochloride
LDC526 HCl
3-[[4-(4-Fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl]amino]benzenemethanesulfonamide hydrochloride
BAY958 HCl
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C17H16FN5O3S · HCl |
Molecular weight | 425.86 |
Biochem/physiol Actions【生化/生理作用】 | 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). |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | 2-8℃ |
SMILES string | FC1=CC=C(C2=NC(NC3=CC(CS(=O)(N)=O)=CC=C3)=NC=N2)C(OC)=C1.Cl |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |