 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1282512-48-4 |
| Molecular formula(MF) | C24H28N8O2 |
| Molecular Weight(MW): | 460.53 |
| Alias |
| In vitro | DMSO | 70 mg/mL warmed (151.99 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL warmed | |
| In vivo |
| Description | GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. | ||||||||||||||||
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| Features | A beta isoform-sparing PI3K inhibitor. | ||||||||||||||||
| Targets |
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| 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. [1] |
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| Cell Data |
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| 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] |