【产品介绍】：

产品名称 Pilaralisib (XL147) 英文名称 Pilaralisib (XL147) 规格或纯度 ≥98% 别名 SAR245408;XL 147 生化机理 Description:IC50 Value:39 nM (PI3Kα); 383 nM (PI3Kβ); 36 nM (PI3Kδ); 23 nM(PI3Kγ) [1]XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values in the nanomolar range in biochemical assays.in vitro: XL147 binds in an ATP-competitive and reversible manner, yet is highly selective against a panel of >130 human protein kinases. In cellular assays, XL147 antagonizes the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) resulting in inhibition of phosphorylation of several downstream effectors of PI3K including Akt, ribosomal S6 kinase, and ribosomal S6 protein [1].Compared with XL147 alone, the combination exhibited a superior antitumor effect against trastuzumab-resistant tumor xenografts. Furthermore, treatment with XL147 and trastuzumab reduced the cancer stem-cell (CSC) fraction within trastuzumab-resistant cells both in vitro and in vivo [2].CAS编号 934526-89-3 溶解性 25°C: DMSO 3 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL 储存温度 储存温度-20°C 分子量 541.02 分子式 C25H25ClN6O4S PubChem CID 56599306