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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. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. The combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032). GDC-0032 is currently in a phase I clinical trial.
| Molecular Weight | 460.53 |
| Formula | C24H28N8O2 |
| CAS Number | 1282512-48-4 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| T-00127-HEV1
T-00127-HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM. |
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
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