LY2857785 free base

产品名称：

1619903-54-6
LY2857785 free base
LY-2857785 free base
N1-[4-(3-isopropyl-2-methyl-indazol-5-yl) pyrimidin-2-yl]-N4-tetrahydropyran-4-yl-cyclohexane-trans-1, 4-diamine
LY 2857785 free base

产品介绍：

产品说明

生化/生理作用

LY2857785 is an ATP-competitive, potent and reversible CDK9/4/8 (IC50 =11 nM/CDK9-CycT, 12 nM/CDK4-CycD1, 16 nM/CDK8-CycC), DYRK2 (IC50 = 44 nM) and FLT3-D835Y (IC50 = 23 nM) inhibitor that significantly reduces cellular RNAP II CTD phosphorylation (U2OS pSer2/pSer5 IC50 =89/42 nM) with good selectivity over a panel of 109 kinase constructs (IC50 = 0.1-1μM/wt FLT3, CDK1/2/3/5/7, PIM1/2; >1 μM/100 kinases). LY2857785 exhibits antiproliferation efficacy in a wide-range cancer cultures (IC50 ∼30 nM-1 μM), and causes AML MV-4-11 xenograft tumor regression in rats (3-9 mg/kg, i.v. infusion Q5Dx5) and mice (8-10 mg/kg, i.v. bolus Q3Dx5) in vivo.

基本信息

经验(实验)分子式	C₂₆H₃₆N₆O
分子量	448.60
MDL编号	MFCD28167812

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	CN1C(C(C)C)=C2C(C=CC(C3=NC(N[C@H]4CC[C@H](NC5CCOCC5)CC4)=NC=C3)=C2)=N1

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