PF-07284892

SKU: orb1944335

Description

PF-07284892 (ARRY-558) is an orally bioavailable, allosteric inhibitor of SHP2 with an IC50 of 21 nM. It suppresses pERK signaling and has demonstrated antitumor activity in preclinical in vitro and in vivo models, supporting its investigation in oncology research for various solid tumors.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 2498597-94-5
• MW: 439.96
• Purity: 97.77% (May vary between batches)
• Formula: C₂₁H₂₂ClN₇S
• SMILES: N[C@H]1C2(CC=3C1=CC=CC3)CCN(CC2)C=4N=CC(SC=5C(Cl)=C(N)N=CC5)=NN4
• Target: Phosphatase,ERK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (7.5 mM);DMSO:80 mg/mL (181.83 mM)

Bioactivity

• Target IC50:
  SHP2:21 nM
• In Vivo:
  After oral administration of 10 mg/kg PF-07284892, the compound exhibited oral bioavailability of 85%, 94%, 102%, and 64% in mice, rats, dogs, and monkeys respectively, demonstrating favorable oral absorption.
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• In Vitro:
  PF-07284892 (100 nM; 4, 18 h), in combination with lorlatinib (0-450 nM) or binimetinib (0-160 nM), reduces pERK expression in H3122 lorR-06 and VACO-432 cells.
  Read more...

Storage & Handling

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

Alternative Names

ARRY558, ARRY-558, PF07284892

Compound Identifiers

PubChem CID

155164064