DC Chemicals Limited
China
Product Name: CNX-2006
Price: $650.0/100mg $1300.0/250mg $2600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1375465-09-0

1375465-09-0 structure

Name: CNX-2006
Chemical Name: N-[3-({2-[(4-{[1-(2-Fluoroethyl)-3-azetidinyl]amino}-2-methoxyphe nyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylam ide
CAS Number: 1375465-09-0
Molecular Formula: C₂₆H₂₇F₄N₇O₂
Molecular Weight: 545.532
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2018-10-07 11:49:20
Modify Date: 2024-01-06 18:43:32
CNX-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
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

Description	CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.
Related Catalog	Research Areas >> Cancer
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	[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

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℃

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