PF-06843195

SKU: orb1693855

Description

PF-06843195 is a selective PI3Kα inhibitor that blocks PIP2 phosphorylation to PIP3, suppressing AKT signaling. It demonstrates anti-tumor efficacy in cellular assays and animal models, supporting its use in oncology research focused on PI3K/AKT pathway dysregulation.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2067281-51-8
• MW: 498.46
• Purity: 98.01% (May vary between batches)
• Formula: C₂₀H₂₅F₃N₈O₄
• SMILES: N([C@]1(CO)CN(C(OCC(F)F)=O)CC1)C=2C(F)=C(N=C(N2)N3CCOCC3)C=4C=NC(N)=NC4
• Target: PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.01 mM);DMSO:50 mg/mL (100.31 mM)

Bioactivity

• Target IC50:
  PI3Kα:0.018 nM (Ki)|PI3Kδ:0.28 nM (Ki)|PI3Kδ:160 nM (IC50, in Rat1 fibroblasts)
• In Vivo:
  Methods: PF-06843195 (10 mg/kg, oral) and (2 mg/kg, intravenous) were used to treat rats and study its pharmacokinetics. Results: It showed excellent bioavailability (25%) after oral administration and high plasma clearance (30 mL/min/kg) and large distribution volume (3.0 L/kg) after intravenous injection.
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• In Vitro:
  PF-06843195 is able to inhibit the proliferation of T47D and MCF7 cells with IC50 values ​​of 32 nM and 62 nM, respectively.

Storage & Handling

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

Alternative Names

PF06843195, PF-06843195, PF 06843195

Compound Identifiers

PubChem CID

124193915