Molecular Formula | C24H28N8O2 |
Molar Mass | 460.53 |
Density | 1.40±0.1 g/cm3(Predicted) |
Boling Point | 783.3±70.0 °C(Predicted) |
pKa | 15.54±0.50(Predicted) |
Storage Condition | 2-8℃ |
In vitro study | GDC-0032 is an orally biopotent, selective inhibitor of the type I PI3Kα,δ, and γ subtypes, inhibiting the PI3Kβ subtype is 30 times less effective than inhibiting the PI3Kα subtype. Pre-clinical data indicate increased activity GDC-0032 against PI3Kα isoform (PIK3CA) mutant and HER2 amplified tumor cell lines. GDC-0032 inhibit MCF7-neo/HER2 cell proliferation with an IC50 of 2.5 nM. |
In vivo study | GDC-0032 pharmacokinetics were dose proportional and time independent, with an average t 1/2 of 40 hours. The combination of GDC-0032 with Fulvestrant, which enhanced Fulvestrant activity, resulted in tumor regression and delayed tumor growth (tumor growth inhibition (TGI) of 91%). In addition, GDC-0032 was combined with Tamoxifen to enhance the efficacy of Tamoxifen in vivo (TGI of the GDC-0032 was 102 percent). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.171 ml | 10.857 ml | 21.714 ml |
5 mM | 0.434 ml | 2.171 ml | 4.343 ml |
10 mM | 0.217 ml | 1.086 ml | 2.171 ml |
5 mM | 0.043 ml | 0.217 ml | 0.434 ml |