CNX-2006

SKU: orb1223328

Description

CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.

Key Properties

• CAS Number: 1375465-09-0
• MW: 545.53
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₇F₄N₇O₂
• SMILES: COc1c(Nc2ncc(c(Nc3cccc(NC(=O)C=C)c3)n2)C(F)(F)F)ccc(NC2CN(CCF)C2)c1
• Target: mTOR
• Solubility: DMSO : ≥ 52 mg/mL. 95.32 mM

Bioactivity

• In Vitro:
  CNX-2006 inhibits EGFR-T790M cells growth up to 1000-fold more compared to wild-type EGFR cells. EGFR inhibition is observed in cells harbouring the T790M mutation at IC50 values below 20 nM after 1 hour exposure to the drug. CNX-2006 also significantly reduces the volume of tumor spheres derived from H1975 cells. CNX-2006 exhibits specificity and potent activity against T790M. The drug also shows activity against uncommon EGFR mutations including G719S, L861Q, an exon 19 insertion mutant (I744-K745insKIPVAI), and T854A, but not an exon 20 insertion (H773-V774HVdup). In an in vitro resistance model, CNX-2006 significantly inhibits the emergence of resistant cells. Chronic exposure to escalating doses of CNX-2006 fails to select for and/or enhance T790M-mediated resistance using PC-9 or HCC827 cells (both harboring exon 19 deletions), or PC-9/ER and HCC827/ER cells with existing T790M and resistance to erlotinib.

Storage & Handling

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

Alternative Names

CNX2006 | CNX 2006 | CNX-2006.

Quick Database Links

Gene Symbol

mTOR