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Chemical Structure| 1375465-09-0 Chemical Structure| 1375465-09-0

Structure of CNX-2006
CAS No.: 1375465-09-0

Chemical Structure| 1375465-09-0

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CNX-2006 is an irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

Synonyms: CNX-2006

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Product Details of CNX-2006

CAS No. :1375465-09-0
Formula : C26H27F4N7O2
M.W : 545.53
SMILES Code : C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
Synonyms :
CNX-2006
MDL No. :MFCD26142654

Safety of CNX-2006

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CNX-2006

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    mutant EGFR, IC50:<20 nM

  • mutant EGFR

    mutant EGFR, IC50:<20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
PC9GR4 61 nM 2 hours Inhibition of EGFR phosphorylation PMC4767465
NCI-H1975 46 nM 2 hours Inhibition of EGFR phosphorylation PMC4767465
HCC-827 55-104 nM 2 hours Inhibition of EGFR phosphorylation PMC4767465
HCC827EPR cells 50 nM to 1 μM 4 months To establish CNX-2006 resistant cell lines and analyze their resistance mechanisms. Results showed that HCC827CNXR S1 cells retained the T790M mutation, while HCC827CNXR S4 cells lost the T790M mutation and acquired MET amplification. PMC4832847

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NCI-H1975 xenograft model Intraperitoneal injection 25 or 50 mg/kg Once daily for 17 days Inhibition of tumor growth PMC4767465

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.17mL

1.83mL

0.92mL

18.33mL

3.67mL

1.83mL

References

 

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