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CNX-2006

Cat. No. M2117
CNX-2006 Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 150  USD150 In stock
25mg USD 270  USD270 In stock
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Quality Control & Documentation
Biological Activity

CNX-2006 is a novel irreversible epidermal growth factor receptor (EGFR) inhibitor. CNX-2006 exhibited specificity and potent in vitro and in vivo activity against T790M. In an in vitro resistance model, CNX-2006 significantly inhibited the emergence of resistant cells compared with erlotinib (1/24 vs 11/24, p = 0.0013). CNX-2006 selectively targets T790M, shows activity against other common and uncommon EGFR mutations, and does not select for resistance mediated by T790M. Additional studies are ongoing to elucidate mechanisms of acquired resistance to CNX-2006.

Chemical Information
Molecular Weight 545.53
Formula C26H27F4N7O2
CAS Number 1375465-09-0
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hiroshi Mizuuchi, et al. Oncogene swap as a novel mechanism of acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitor in lung cancer

[2] Elena Galvani, et al. NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor

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Keywords: CNX-2006 supplier, EGFR/HER2, inhibitors, activators


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