产品说明
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).
基本信息
经验(实验)分子式 | C17H16FN5O3S · HCl |
分子量 | 425.86 |
产品性质
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
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
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |