| 货号： | ONI-171725 |
| CAS号： | 934526-89-3 |
| 供应商： | 美国 |
| 数量： | 1224.0 |
| 英文名： | XL-147; SAR245408,XL147,XL 147,SAR-245408,SAR 245408 |
| 保质期： | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| 保存条件： | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| 规格： | (5mg/100mg/774mg) |
XL147(SAR245408; pilaralisib) is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM/383 nM/36 nM/23 nM for PI3Kα/β/δ/γ, respectively; less potent to PI3Kβ. IC50 Value:39 nM (PI3Kα); 383 nM (PI3Kβ); 36 nM (PI3Kδ); 23 nM(PI3Kγ) [1] Target: 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]. in vivo: SAR245408 induced significant differences in EFS distribution compared to control in 29 of 37 (79%) of solid tumor xenografts and in two of seven (29%) ALL. Xenografts. SAR245408 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity (EFS T/C?>?2) in 4 of 37 (11%) solid tumor xenografts [3]. Toxicity: In vitro SAR245408 demonstrated cytotoxic activity, with a median relative IC50 value of 10.9??M (range 2.7-24.5??M) [4]. Clinical trial: Open-label Treatment Extension Study With SAR-245408 or SAR-245409 as a Monotherapy or as a Combination Regimen. Phase 1/Phase 2
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