CAS:663619-89-4TGX-221

您的位置 : 首页 / PI3K/Akt/mTOR / PI3K / TGX-221

TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, and is 1000-fold selective for p110β than p110α.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

663619-89-4

储存条件

分子式

C21H24N4O2

运输

蓝冰

分子量

364.44

别名

溶解度

DMSO	33.0 mg/mL (90.5 mM) warming
Water	insoluble

动物实验配方

IP	3% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

生物活性

描述Phosphatidylinositol 3-kinases (PI3Ks) are a family of enzymes that catalyse the phosphorylation of phosphatidylinositol at the 3′-position of the inositol ring, producing secondary messenger lipids which control cellular activities including survival, growth and proliferation. These lipid kinases are divided into three distinct classes (Class I, II and III), Class I PI3Ks are heterodimers which consist of one of four closely related catalytic p110 subunits (α, β, δ and γ) and an associated regulatory subunit (p85/p55). TGX-221 is an selective p110β inhibitor, with more than 1000 fold selectivity over the related p110α isoform. TGX-221 can also inhibit the phosphorylation level of its downstream signal. The (R)-enantiomer of TGX-221 (1a) was eventually identified as the bioactive form against the p110β-isoform (IC50 = 6nM and 800nM for the R and S stereoisomers, respectively). In a vitro study, treatment with 50 - 150 µM TGX-221 for 48h can significantly inhibited the viability of U87 and U251 cells. The IC50 values of TGX-221 in U87 and U251 cells were ~40 and 100 µM, respectively.
动物研究
剂量
Rat: 2.5 mg/kg, 25 mg/kg^[3] (i.v.) Mice: 10 mg/kg^[4] (i.p.), 40 mg/kg^[5] (i.p.); 6.25 mg/kg - 100 mg/kg^[6] (i.v.)

给药途径
i.v., i.p.

动物研究
剂量	Rat: 2.5 mg/kg, 25 mg/kg^[3] (i.v.) Mice: 10 mg/kg^[4] (i.p.), 40 mg/kg^[5] (i.p.); 6.25 mg/kg - 100 mg/kg^[6] (i.v.)
给药途径	i.v., i.p.