Mavelertinib

SKU: orb1705133

Description

Mavelertinib (PF-06747775) is a potent, orally bioavailable, and selective EGFR tyrosine kinase inhibitor targeting oncogenic mutants including T790M/L858R and T790M/Del. It is a research tool for investigating non-small cell lung cancer (NSCLC), with demonstrated activity in both cellular assays and in vivo xenograft models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1776112-90-3
• MW: 415.42
• Purity: 99.89%
• Formula: C₁₈H₂₂FN₉O₂
• SMILES: COc1nn(C)cc1Nc1nc(nc2n(C)cnc12)N1C[C@@H](F)[C@@H](C1)NC(=O)C=C
• Target: EGFR
• Solubility: H2O:<0.1 mg/mL;DMSO:30 mg/mL (72.22 mM)

Bioactivity

• Target IC50:
  EGFR (WT):307 nM|ERG26 current (human):＞100 μM|Del:5 nM|T790M/L858R:12 nM|T790M/Del:3 nM|L858R:4 nM
• In Vivo:
  Following oral administration (1 mg/kg to mouse, rat, and dog), Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%). Due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg), Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) following intravenous administration.
• In Vitro:
  Inhibiting the hERG26 current with an IC50 greater than 100 μM, Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM). With less than 50% effect or inhibition against all nonkinase targets at 10 μM, Mavelertinib demonstrates its selectivity.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PFE-X775, PF6747775, PF-6747775, PF-7775, PF06747775, PF-06747775, PF 6747775, PF 06747775, EGFR (T790M/L858R), Mavelertinib

Compound Identifiers

PubChem CID

91668194