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GDC-0032

(CAS No:1282512-48-4)
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.
CAS No:1282512-48-4
Molecular Weight(MW):460.53
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1282512-48-4
Molecular formula(MF) C24H28N8O2
Molecular Weight(MW): 460.53
Alias
Solubility
In vitro DMSO 70 mg/mL warmed (151.99 mM)
Water <1 mg/mL
Ethanol <1 mg/mL warmed
In vivo
Biological Activity
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.
Features A beta isoform-sparing PI3K inhibitor.
Targets
PI3Kδ [1] PI3Kα [1] PI3Kγ [1] PI3Kβ [1] C2β [1]
0.12 nM(Ki) 0.29 nM(Ki) 0.97 nM(Ki) 9.1 nM(Ki) 292 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MOLM16 cells Proliferation assay 72 h Antiproliferative activity against human MOLM16 cells after 72 hrs by Cell Titer-Blue assay 22727640

... Click to View More Cell Line Experimental Data

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]