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CAS No.: 663619-89-4

TGX-221 Catalog No. CSN12315

Synonyms: 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	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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)^[3]. 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^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
DU145	-	Growth Inhibition Assay	-	IC50=35.6 ± 0.12 μM	22494444
HUVECs	500 nM	Function Assay	1 h	reduces Akt phosphorylation	22814170
LNCaP	-	Growth Inhibition Assay	-	IC50=3.98 ± 0.18 μM	22494444

更多
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.
参考文献

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.

[1] Zhao Y, Duan S, et al. Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells. Mol Pharm. 2012 Jun 4;9(6):1705-16.
[2] Straub A, Wendel HP, et al. Selective inhibition of the platelet phosphoinositide 3-kinase p110beta as promising new strategy for platelet protection during extracorporeal circulation. Thromb Haemost. 2008 Mar;99(3):609-15.
[3] Marshall AJ, Lill CL, Chao M, Kolekar SV, Lee WJ, Marshall ES, Baguley BC, Shepherd PR, Denny WA, Flanagan JU, Rewcastle GW. Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling. Bioorg Med Chem. 2015 Jul 1;23(13):3796-808. doi: 10.1016/j.bmc.2015.03.073. Epub 2015 Apr 4. PMID: 25890698.
[4] Yang X, Yang JA, Liu BH, Liao JM, Yuan FE, Tan YQ, Chen QX. TGX-221 inhibits proliferation and induces apoptosis in human glioblastoma cells. Oncol Rep. 2017 Nov;38(5):2836-2842. doi: 10.3892/or.2017.5991. Epub 2017 Sep 22. PMID: 29048665; PMCID: PMC5780035.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7439 mL
- 13.7196 mL
- 27.4393 mL
- 5 mM
- 0.5488 mL
- 2.7439 mL
- 5.4879 mL
- 10 mM
- 0.2744 mL
- 1.3720 mL
- 2.7439 mL

技术信息

CAS号

663619-89-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H24N4O2

运输

蓝冰

分子量

364.44

别名

TGX-221

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

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