EGFR-IN-11

• CAT Number: I017547
• CAS Number: 2463200-44-2
• Molecular Formula: C₂₉H₃₅N₉O₂S
• Molecular Weight: 573.71
• Purity: ≥95%
• Storage: Store at -20°C
• IUPAC Name: 9-[(3R)-1-cyclopropylsulfonylpyrrolidin-3-yl]-2-N-[4-(4-methylpiperazin-1-yl)phenyl]-8-N-phenylpurine-2,8-diamine
• InChI: InChI=1S/C29H35N9O2S/c1-35-15-17-36(18-16-35)23-9-7-22(8-10-23)31-28-30-19-26-27(34-28)38(29(33-26)32-21-5-3-2-4-6-21)24-13-14-37(20-24)41(39,40)25-11-12-25/h2-10,19,24-25H,11-18,20H2,1H3,(H,32,33)(H,30,31,34)/t24-/m1/s1
• InChIKey: RNEHWYIFHKBZAW-XMMPIXPASA-N
• SMILES: CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4C(=N3)N(C(=N4)NC5=CC=CC=C5)C6CCN(C6)S(=O)(=O)C7CC7

EGFR-IN-11 (Cat No.:I017547) is a potent and selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 3.1 nM. It shows excellent selectivity against other related kinases such as HER2, HER4, and VEGFR-2. EGFR-IN-11 has been reported to induce growth arrest and apoptosis in EGFR-dependent tumor cells and suppress tumor growth in xenograft models. It may be a potential therapeutic agent for the treatment of EGFR-dependent cancers.

Reference

[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.