Antibodies
WZ8040
- 貨號 Cat. No.
- S1179
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
WZ8040
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
| Size | Price | Stock | Quantity | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||||||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). | |||||
|---|---|---|---|---|---|---|
| Targets | EGFR T790M | |||||
| IC50 | ||||||
| In vitro | WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. [1] | |||||
| In vivo | ||||||
| Features | Inhibits EGFR T790M mutation and not wild-type EGFR. | |||||
Protocol(Only for Reference)
Cell Assay: [1]
| Cell lines | HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3 |
|---|---|
| Concentrations | Dissolved in DMSO, final concentrations ~10 μM |
| Incubation Time | 72 hours |
| Method | Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay. |
References
Chemical Information
| Molecular Weight (MW) | 481.01 |
|---|---|
| Formula | C24H25ClN6OS |
| CAS No. | 1214265-57-2 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 96 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 3 mg/mL (6 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 | N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.48101 | 4.8101 | 9.6202 | 14.4303 |
Customer Reviews (2)
 Click to enlarge | Rating | |
| Source | Dr. Zhang of Tianjin Medical University. WZ8040 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | A549 cells | |
| Concentrations | 0-1 μM | |
| Incubation Time | 3 h | |
| Results | WZ8040 treatment resulted in a reduction of AKT phosphorylation in A549 cells. |
