| 产品描述： | p110δ 选择性抑制剂;p110δ Selective Inhibitors;;InformationTaselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targetingPI3Kα/δ/γwithKiof 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.TargetsPI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay); C2β (Cell-free assay) 14554,0.12 nM(Ki); 0.29 nM(Ki); 0.97 nM(Ki); 9.1 nM(Ki); 292 nMIn vitroGDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM.In vivoGDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032).Cell Research(from reference)Cell lines：MCF7-neo/HER2 Cells Incubation Time：3 and 4 days |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京