PF-04979064, PI3K/mTOR Dual Inhibitor


Catalog No. size PriceQuantity
M60114-2S 2 mg solid $149
M60114-10S 10mg solid $596

Description

Product Information
Molecular Weight: 446.5
Formula: C24H26N6O3
Purity: ≥98%
CAS#: 1220699-06-8
Solubility: DMSO up to 100 mM
Chemical Name: (S)-1-(1-(2-hydroxypropanoyl)piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1H-imidazo[4,5-c][1,5]naphthyridin-2(3H)-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor developed through structure-based drug design. It inhibited mTOR, PI3Kα, β, δ and γ isoforms and AKT phosphorylation with IC50 as 2.64 nM, 0.395 nM, 0.111 nM, 0.122 nM and 28.3 nM, respectively. PF-04979064 exhibited cellular potency with an IC50 of 9.1 nM in a BT20 cell assay. PF-04979064 exhibited excellent in vitro potency, very good solubility, high LipE, excellent kinome selectivity, robust PK/PD correlation and tumor growth inhibition (TGI) in a U87MG mouse xenograft model, and acceptable predicted human clearance after incorporating both CYP- and AO-mediated metabolism. PF-04979064 is the back-up candidate to PF-04691502 which is in Phase I/II clinical trials for treating solid tumors.

 


How to Use:

 

 

  • In vitro: PF-04979064 was used at 1-10 µM in vitro and in cellular assays.
  • In vivo: PF-04979064 was orally dosed to mice at 15-40 mg/kg once per day for two weeks.

 

 

 

Reference:

 

  1. Hengmiao Cheng, et al. Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. (2013) ACS Med. Chem. Lett., 4 (1), pp91-97.

 

 


 

Products are for research use only. Not for human use.

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