Antibodies
CNX-2006
- 貨號 Cat. No.
- S7206
- 規格 Size
- 5 mgã€25 mg
- 品牌 Brand
- Selleckchem
Description
CNX-2006
Catalog No.S7206
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. | |||||
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| Targets | mutant EGFR | |||||
| IC50 | < 20 nM[1] | |||||
| In vitro | 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. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2] | |||||
| In vivo | CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Growth inhibition assays | Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. |
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Cell Assay: [1]
| Cell lines | HEK293 |
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| Concentrations | ~1000 nM |
| Incubation Time | 6 h |
| Method | 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. |
Animal Study: [2]
| Animal Models | Nude mice |
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| Dosages | 25 mg/kg |
| Administration | i.p. |
References
Chemical Information
| Molecular Weight (MW) | 545.53 |
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| Formula | C26H27F4N7O2 |
| CAS No. | 1375465-09-0 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (183 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 29 mg/mL (53 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 2-Propenamide, N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- |
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