CNX-2006

SKU: orb1301177

Description

CNX-2006

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1375465-09-0
• MW: 545.53
• Purity: 98.85%
• Formula: C₂₆H₂₇F₄N₇O₂
• SMILES: COc1cc(NC2CN(CCF)C2)ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F
• Target: EGFR
• Solubility: DMSO:91 mg/mL (166.81 mM);DMF:soluble

Bioactivity

• Target IC50:
  EGFR (mutant):<20 nM
• In Vivo:
  CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
• In Vitro:
  CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.
• Cell Research:
  Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.(Only for Reference)
• Animal Research:
  Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p.

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

CNX 2006, CNX2006, CNX-2006, inhibit, Inhibitor, HER1, Epidermal growth factor receptor, EGFR, EGFR (mutant), ErbB-1

Compound Identifiers

PubChem CID

56968072