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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-Pilaralisib
Pilaralisib

Chemical Structure : Pilaralisib

CAS No.: 934526-89-3

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Pilaralisib (XL-147, SAR245408, XL147, SAR-245408)

货号: PC-28709Not For Human Use, Lab Use Only.

Pilaralisib (XL147, SAR245408) is a potent and highly selective, orally active class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pilaralisib (XL147, SAR245408) is a potent and highly selective, orally active class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively.
Pilaralisib (XL147, SAR245408) shows broad kinase selectivity profiling of >130 protein kinases.
Pilaralisib (XL147, SAR245408) inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 in multiple tumor cell lines with diverse genetic alterations affecting the PI3K pathway in cellular assays.
Pilaralisib (XL147, SAR245408) inhibits proliferation with a wide range of potencie in a panel of tumor cell lines.
Pilaralisib (XL147, SAR245408) induces dose-dependent inhibition of phosphorylation of AKT, p70S6K, and S6 with a duration of action of at least 24 hours in mouse xenograft models, causes significant tumor growth inhibition in multiple human xenograft models in nude mice.

物理化学性质&存储条件

分子量 541.02
分子式 C25H25ClN6O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Amino-N-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide

参考文献

1. Foster P, et al. Mol Cancer Ther. 2015 Apr;14(4):931-40.

2. Chakrabarty A, et al. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2718-23.

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