PF-04979064

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性的双重 PI3K/mTOR 抑制剂。

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.

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.

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%.

PF 04979064 | PF04979064

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

——

1220699-06-8

446.5016

C24H26N6O3

>98% (HPLC)

DMSO: 11 mg/mL

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

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)-

(-20℃)

With Ice Pack

≥ 2 years