CHMFL-EGFR-202

SKU: orb1710058

Description

CHMFL-EGFR-202 is a potent, irreversible EGFR kinase inhibitor, effective against both wild-type and drug-resistant T790M mutant forms with IC50 values of 8.3 nM and 5.3 nM, respectively. It is a valuable research tool for in vitro and in vivo studies targeting EGFR-driven cancers, including non-small cell lung cancer.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2089381-40-6
• MW: 489.96
• Purity: 99.66%
• Formula: C₂₅H₂₄ClN₇O₂
• SMILES: NC1=C2C(=NN(C2=NC=N1)[C@H]3CN(C(C=C)=O)CCC3)C4=CC(Cl)=C(OCC5=CC=CC=N5)C=C4
• Target: MEK,BTK,EGFR
• Solubility: DMSO:45 mg/mL (91.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.08 mM)

Bioactivity

• Target IC50:
  EGFR:8.3 nM|EGFR (T790M):5.3 nM|BLK:8.1 nM|BTK:24.5 nM|ERB4:3.2 nM|MEK1:161 nM|BMX kinase:111 nM|ErbB2:8.1 nM
• 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).

Storage & Handling

• Storage: 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

CHMFL EGFR 202, CHMFL-EGFR 202, CHMFLEGFR202, CHMFL-EGFR202, CHMFL-EGFR-202, BMX, Btk, BLK, ErbB4, ErbB2, EGFR, EGFRT790M, MEK1

Compound Identifiers

PubChem CID

127264586