PF-04979064

SKU: orb1226766

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.

Key Properties

• CAS Number: 1220699-06-8
• MW: 446.5016
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₆N₆O₃
• SMILES: CC1=NC=C(C=C1)C2=NC3=C4C(=CN=C3C=C2)N(C(=O)N4C5CCN(CC5)C(=O)C(C)O)C
• Target: PI3K
• Solubility: DMSO: 11 mg/mL

Bioactivity

• 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%.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PF 04979064 | PF04979064

Quick Database Links

Gene Symbol

PI3K