PF-04979064( PF 04979064 | PF04979064 )

Catalog No. M10834 CAS No. 1220699-06-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-04979064
Note

Research use only, not for human use.
Brief Description

A highly potent and selective, dual PI3K/mTOR inhibitor.
Description

A highly potent and selective, dual PI3K/mTOR inhibitor with Ki of 0.13, 0.111, 0.122 and 1.42 nM for PI3Kα, PI3Kγ, PI3Kδ and mTOR, respectively; exhibits excellent in vitro potency, very good solubility, high LipE, excellent kinome selectivity, robust PK/PD correlation and TGI efficacy, and acceptable predicted human clearance after incorporating both CYP- and AO-mediated metabolism.
In Vitro

PF-04979064 is tested against human class I PI3K isoforms PI3Kα, PI3Kγ, and PI3Kδ, with PI3Kα Ki of 0.13 nM, PI3Kγ Ki of 0.111 nM, and PI3Kδ Ki of 0.122 nM.
In Vivo

PF-04979064 is progressed to rat in vivo PK studies and exhibits robust PK profile: Vdss=5.23 L/kg, Cl=19.3 mL/min/kg, T1/2=1.85 h, and F%=61%.
Synonyms

PF 04979064 | PF04979064
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3K
Research Area

Cancer
Indication

——

CAS Number

1220699-06-8
Formula Weight

446.5016
Molecular Formula

C24H26N6O3
Purity

>98% (HPLC)
Solubility

DMSO: 11 mg/mL
SMILES

CC1=NC=C(C=C1)C2=NC3=C4C(=CN=C3C=C2)N(C(=O)N4C5CCN(CC5)C(=O)C(C)O)C
Chemical Name

2H-Imidazo[4,5-c][1,5]naphthyridin-2-one, 1,3-dihydro-1-[1-[(2S)-2-hydroxy-1-oxopropyl]-4-piperidinyl]-3-methyl-8-(6-methyl-3-pyridinyl)-

1. Cheng H, et al. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7.

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