Taselisib（GDC-0032） — Datasheet

Biological Activity

GDC-0032 is a potent, next-generation β iso Form-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. IC50 Value: 0.29 nM/0.12 nM /0.97 nM(PI3Kα/δ/γ) Target: PI3K in vitro: GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ iso Forms, with 30 fold less inhibition of the PI3K β iso Form relative to the PI3Kα iso Form. Preclinical data show that GDC-0032 has increased activity against PI3Kα iso Form (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. in vivo: GDC-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) .For the detailed information of GDC-0032, the solubility of GDC-0032 in water, the solubility of GDC-0032 in DMSO, the solubility of GDC-0032 in PBS buffer, the animal experiment (test) of GDC-0032, the cell expriment (test) of GDC-0032, the in vivo, in vitro and clinical trial test of GDC-0032, the EC50, IC50,and Affinity of GDC-0032, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.