Introduction：Basic information about CAS 1375465-09-0|CNX-2006, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | CNX-2006 |
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| CAS Number | 1375465-09-0 | Molecular Weight | 545.532 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C26H27F4N7O2 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| 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 |
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CNX-2006 BiologicalActivity
| 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 | Research Areas >>Cancer |
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| Target | EGFRT790M:20 nM (IC50) EGFRL858R/T790M |
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| 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]. |
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| References | [1]. Galvani E, et al. Abstract 3244: Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX-2006, a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC. CNX-2006, a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 3244. doi:10.1158/1538-7445.AM2013-3244 [2]. Ohashi K, et al. Abstract 2101A: CNX-2006, a novel irreversible epidermal growth factor receptor (EGFR) inhibitor, selectively inhibits EGFR T790M and fails to induce T790M-mediated resistance in vitro. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 2101A. doi:10.1158/1538-7445.AM2013-2101A |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C26H27F4N7O2 |
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| Molecular Weight | 545.532 |
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| Exact Mass | 545.216248 |
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| PSA | 110.16000 |
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| LogP | 2.28 |
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| Index of Refraction | 1.643 |
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| InChIKey | BFSRTTWIPACGMI-UHFFFAOYSA-N |
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| SMILES | C=CC(=O)Nc1cccc(Nc2nc(Nc3ccc(NC4CN(CCF)C4)cc3OC)ncc2C(F)(F)F)c1 |
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| Storage condition | -20℃ |
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Synonyms
| 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 |
