您的位置:首页 > 产品中心 > 853299-07-7, K03861
K03861
产品别名
853299-07-7
K03861
1-[4-(2-Aminopyrimidin-4-yloxy)phenyl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-trifluoromethylphenyl]urea
AUZ454
CCG 269702
AUZ 454
K-03861
AUZ-454
CCG269702
K 03861
CCG-269702
N-[4-[(2-Amino-4-pyrimidinyl)oxy]phenyl]-N′-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]urea
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C24H26F3N7O2 |
Molecular weight | 501.50 |
MDL number | MFCD19443769 |
Biochem/physiol Actions【生化/生理作用】 | K03861 is an ATP site-binding, cyclin-competitive, type II CDK2 inhibitor that selectively targets and locks the kinase in its inactive DFG-out conformation (CDK2 Kd = 50 nM, DFG-out stabilizing CDK2-C118L/A144C mutant Kd = 9.7 nM without vs. 134.1 nM with bound cycB; CDK2-C118L/A144C-cycA IC50 = 0.8 μM), rendering it incompatible for cyclin bining. K03861 selectively inhibits CDK2-C118L/A144C over CycA-bound wt CDK2 by in vitro kinase assay (IC50 = 0.8 vs. >10 μM) and inhibits the proliferation of immortalized multipotent otic progenitor (iMOP) murine cell line (by 81% and 92%, resepectively, at 0.1 and 1.0 μM). |
产品性质
Quality Level【质量水平】 | 100 |
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】 | −20℃ |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |