GDC-0032|cas 1282512-48-4| DC Chem|Supplier|Price|Buy  

GDC-0032|cas 1282512-48-4| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: GDC-0032, Cas: 1282512-48-4 ,Cat No. DC7416, Purity>98%, In stock.

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GDC-0032|cas 1282512-48-4, Synonym name: GDC0032; GDC 0032, Chemical name:　, Molecule weight: 460.53, Molecule Formula: C24H28N8O2

GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

GDC-0032 is a potent, next-generation β isoform-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) [1]

Target: PI3K

in vitro: GDC-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 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) [1].