CHMFL-EGFR-202

SKU: orb1940806

Description

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases).(In Vitro):CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. CHMFL-EGFR-202 displays strong binding affinities against wild-type, L861Q, G719C/S, L858R/T790M, L858R, and T790M among EGFR wild-type and mutant kinases. CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM). CHMFL-EGFR-202 strongly inhibits BLK, BTK, ERBB2 and ERBB4 (IC50s: of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM). CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases (IC50s: 111.0 nM and 161.0 nM).

Key Properties

• CAS Number: 2089381-40-6
• MW: 489.96
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₄ClN₇O₂
• SMILES: Nc1ncnc2n(nc(-c3ccc(OCc4ccccn4)c(Cl)c3)c12)[C@@H]1CCCN(C1)C(=O)C=C
• Target: EGFR

Bioactivity

• In Vitro:
  CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. CHMFL-EGFR-202 displays strong binding affinities against wild-type, G719C/S, L858R, L858R/T790M, L861Q, and T790M among EGFR wild-type and mutant kinases. CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM). CHMFL-EGFR-202 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively. CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50 of 111.0 nM and 161.0 nM.

Storage & Handling

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

Quick Database Links

Gene Symbol

EGFR