Pilaralisib

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Chemical Structure| 934526-89-3 同义名 : XL147
CAS号 : 934526-89-3
货号 : A205476
分子式 : C25H25ClN6O4S
纯度 : 99%
分子量 : 541.02
MDL号 : MFCD26142605
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°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
描述 XL147 (SAR245408, pilaralisib), an ATP-competitive pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, is a promising new anticancer drug. XL147 reversibly binds to p110α, p110β, p110γ, and p110δ with half-maximal inhibitory concentration (IC50) values of 48, 617, 10, and 260 nM, respectively, and has been reported to show an inhibitory effect on the growth of various cancer cell lines in a dose-dependent manner. In addition, XL147 strongly inhibited the PI3K/AKT/mTOR pathway in tumor xenograft models and displayed robust antitumor activity in tumor-bearing mice[3]. Administration of XL147 at oral doses of 10, 30, 100, or 300 mg/kg on xenograft mice caused a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors harvested 4, 24, or 48h, postdose, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4h[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.24mL

1.85mL

0.92mL

18.48mL

3.70mL

1.85mL
参考文献

[1]Foster P, Yamaguchi K, et al. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40.

[2]Reynolds CP, Kang MH, et al. Initial testing (stage 1) of the phosphatidylinositol 3' kinase inhibitor, SAR245408 (XL147) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2013 May;60(5):791-8.

[3]Chakrabarty A, Sánchez V, Kuba MG, Rinehart C, Arteaga CL. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2718-23. doi: 10.1073/pnas.1018001108. Epub 2011 Feb 28. PMID: 21368164; PMCID: PMC3286932.

[4]Foster P, Yamaguchi K, Hsu PP, Qian F, Du X, Wu J, Won KA, Yu P, Jaeger CT, Zhang W, Marlowe CK, Keast P, Abulafia W, Chen J, Young J, Plonowski A, Yakes FM, Chu F, Engell K, Bentzien F, Lam ST, Dale S, Yturralde O, Matthews DJ, Lamb P, Laird AD. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40. doi: 10.1158/1535-7163.MCT-14-0833. Epub 2015 Jan 30. PMID: 25637314.