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CAS No.: 1007207-67-1

Izorlisib Catalog No. CSN15797

Synonyms: CH5132799;PA-799

CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM, and is less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines.

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400-920-2911

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tech@csnpharm.cn

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The deregulation of phosphatidylinositol 3-kinase (PI3K)/Akt pathway is commonly seen in various human cancers. CH5132799 is a PI3K inhibitor that inhibits PI3Kα, β, δ, γ with IC50 values of 14 nM, 0.12 mM, 0.5 mM and 36 nM, respectively. In breast cancer KPL-4 cells harboring PIK3CA mutation, treatment of 0.001 – 10 mM CH5132799 for 2h suppressed the phosphorylation of Akt and its downstream factors, S6K, S6 and 4E-BP1. When KPL-4 cells were treated with 1 mM CH5132799 for 48h, the G₁ arrest and Caspase 3/7 activity were induced. CH5132799 also demonstrated anti-proliferative effect in 60 breast, ovarian, prostate, and endometrial cancer cell lines with 75% of lines having an IC50 value less than 1mM and 38% of lines having an IC50 under 0.3 mM. In the xenograft model of KPL-4 cells harboring the PIK3CA H1047R mutation, daily oral administration of CH5132799 (0.39 – 25 mg/kg/day) showed anti-tumor effect since day 21 post tumor implantation. The inhibition of the PI3K pathway and Akt phosphorylation were also observed in this xenografts model treated by CH5132799. Oral administration of CH5132799 (12.5 mg/kg/day, 12 consecutive days) in mice bearing trastuzumab-insensitive KPL-4 tumors induced remarkable reduction in the tumor volume, and eventually the disappearance of the tumors^[3].
作用机制CH5132799 is a selective, ATP-competitive inhibitor of class I PI3K that interacts with the ATP-binding site of PI3K^[3].
动物研究
剂量
Mice: 0.39 mg/kg - 25 mg/kg (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 0.39 mg/kg - 25 mg/kg (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01222546	Solid Tumors	Phase 1	Completed	-	United Kingdom ... more >> Investigator Sites London, Leeds, United Kingdom Collapse <<

参考文献

[1] Tanaka H, Yoshida M, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
[2] Ohwada J, Ebiike H, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. doi: 10.1016/j.bmcl.2011.01.065. Epub 2011 Jan 22.
[3] Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, Ohwada J, Ebiike H, Kuramoto S, Morita K, Yoshimura Y, Yamazaki T, Ishii N, Kondoh O, Aoki Y. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.

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
- 2.6496 mL
- 13.2478 mL
- 26.4956 mL
- 5 mM
- 0.5299 mL
- 2.6496 mL
- 5.2991 mL
- 10 mM
- 0.2650 mL
- 1.3248 mL
- 2.6496 mL

技术信息

CAS号

1007207-67-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H19N7O3S

运输

蓝冰

分子量

377.42

别名

CH5132799;PA-799

溶解度

DMSO	12.0 mg/mL (31.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

1% DMSO+30% polyethylene glycol+1% Tween 80+water

30 mg/mL

suspension

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