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GDC-0032

Cat. No. M2135
GDC-0032 Structure
Synonym:

Taselisib; RG-7604

Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 460.53
Formula C24H28N8O2
CAS Number 1282512-48-4
Purity >98%
Solubility DMSO
Storage at -20°C
References

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Ndubaku CO, et al. J Med Chem. 2013 Jun 13;56(11):4597-610. PMID: 23662903.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GDC-0032, Taselisib; RG-7604 supplier, PI3K, inhibitors

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