Description
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.
Product information
CAS Number: 1220699-06-8
Molecular Weight: 446.50
Formula: C24H26N6O3
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
Smiles: CN1C2=CN=C3C=CC(=NC3=C2N(C2CCN(CC2)C(=O)[C@H](C)O)C1=O)C1=CN=C(C)C=C1
InChiKey: GACQNUHFDBEIQH-HNNXBMFYSA-N
InChi: InChI=1S/C24H26N6O3/c1-14-4-5-16(12-25-14)18-6-7-19-21(27-18)22-20(13-26-19)28(3)24(33)30(22)17-8-10-29(11-9-17)23(32)15(2)31/h4-7,12-13,15,17,31H,8-11H2,1-3H3/t15-/m0/s1
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
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.
References:
- 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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