CAS NO: | 1375465-09-0 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 545.53 |
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Formula | C26H27F4N7O2 |
CAS No. | 1375465-09-0 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 100 mg/mL (183.3 mM) |
Water: <1 mg/mL | |
Ethanol: 29 mg/mL (53.1 mM) | |
Other info | Chemical Name: N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide InChi Key: BFSRTTWIPACGMI-UHFFFAOYSA-N InChi Code: InChI=1S/C26H27F4N7O2/c1-3-23(38)33-16-5-4-6-17(11-16)34-24-20(26(28,29)30)13-31-25(36-24)35-21-8-7-18(12-22(21)39-2)32-19-14-37(15-19)10-9-27/h3-8,11-13,19,32H,1,9-10,14-15H2,2H3,(H,33,38)(H2,31,34,35,36) 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; CNX 2006; CNX2006. |
In Vitro | In vitro activity: CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9. Kinase Assay: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. Cell Assay: Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting. |
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In Vivo | CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. |
Animal model | Nude mice |
Formulation & Dosage | 5% DMSO:15% Solutol HS15 in PBS; 25 mg/kg; i.p. |
References | Galvani E, Sun J, Leon LG, et al. Oncotarget, 2015. |