GSK2636771

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Chemical Structure| 1372540-25-4 同义名 : -
CAS号 : 1372540-25-4
货号 : A169634
分子式 : C22H22F3N3O3
纯度 : 99%
分子量 : 433.42
MDL号 : MFCD22417098
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • p110β
描述 The PI3K/protein kinase B (AKT) pathway is commonly activated in several tumor types. Selective targeting of p110β could result in successful pathway inhibition while avoiding the on- and off-target effects of pan-PI3K inhibitors. GSK2636771 is a potent, orally bioavailable, adenosine triphosphate-competitive, selective inhibitor of PI3Kβ with IC50s of 3.5 nM, 20.49 nM, 40.53 nM for p110α p110β and p110γ, respectively[3]. In a vivo study, female nude mice with tumor xenografts were treated with vehicle or GSK2636771 at 1, 3, 10, or 30 mg/kg by oral gavage for 21 days and GSK2636771 resulted in tumor growth inhibition. In a cell study, C4-2B cells and its MDV3100-resistant subline was pretreated with GSK2636771 range from 1-100μM in 30mins. The result showed that treatment with GSK2636771 significantly increased G0/G1 population accompanied with a large reduction of S-phase cells not only in C4-2B cells but also in C4-2B/MDV-R cells, although the extent of G1/G0 phase arrest in MDV-R cells was less than that in the parental C4-2B cells[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL
参考文献

[1]Leroy C, Ramos P, et al. Activation of IGF1R/p110β/AKT/mTOR confers resistance to α-specific PI3K inhibition. Breast Cancer Res. 2016 Apr 5;18(1):41.

[2]Weigelt B, Warne PH, et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.

[3]Mateo J, Ganji G, Lemech C, Burris HA, Han SW, Swales K, Decordova S, DeYoung MP, Smith DA, Kalyana-Sundaram S, Wu J, Motwani M, Kumar R, Tolson JM, Rha SY, Chung HC, Eder JP, Sharma S, Bang YJ, Infante JR, Yan L, de Bono JS, Arkenau HT. A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors. Clin Cancer Res. 2017 Oct 1;23(19):5981-5992. doi: 10.1158/1078-0432.CCR-17-0725. Epub 2017 Jun 23. PMID: 28645941.

[4]He C, Duan S, Dong L, Wang Y, Hu Q, Liu C, Forrest ML, Holzbeierlein JM, Han S, Li B. Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells. Prostate. 2017 Aug;77(11):1187-1198. doi: 10.1002/pros.23377. Epub 2017 Jun 20. PMID: 28631436; PMCID: PMC5527967.