CNX-2006
Modify Date: 2024-01-06 18:43:32
CNX-2006 structure
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Common Name | CNX-2006 | ||
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| CAS Number | 1375465-09-0 | Molecular Weight | 545.532 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C26H27F4N7O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CNX-2006CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M. |
| Name | N-[3-({2-[(4-{[1-(2-Fluoroethyl)-3-azetidinyl]amino}-2-methoxyphe nyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylam ide |
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| Synonym | More Synonyms |
| Description | CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M. |
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| Related Catalog | |
| Target |
EGFRT790M:20 nM (IC50) EGFRL858R/T790M |
| 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[1]. 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[2]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C26H27F4N7O2 |
| Molecular Weight | 545.532 |
| Exact Mass | 545.216248 |
| PSA | 110.16000 |
| LogP | 2.28 |
| Index of Refraction | 1.643 |
| Storage condition | -20℃ |
| 2-Propenamide, N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- |
| N-[3-({2-[(4-{[1-(2-Fluoroethyl)-3-azetidinyl]amino}-2-methoxyphenyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylamide |
| CNX2006 |
| CNX-2006 |