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WZ8040
🥰Excellent
Catalog No. T6734Cas No. 1214265-57-2
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
WZ8040
🥰Excellent
Purity: 97.42%
Catalog No. T6734Cas No. 1214265-57-2
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $40 | In Stock | |
| 5 mg | $95 | In Stock | |
| 10 mg | $153 | In Stock | |
| 25 mg | $259 | In Stock | |
| 50 mg | $385 | In Stock | |
| 100 mg | $567 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock |
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Purity:97.42%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). |
| Targets&IC50 | H1819 (ErbB2 amp):738 nM , HCC827 (EGFR Del E746_A750):1 nM, H1975 (EGFR L858R/T790M):9 nM, HCC827 GR (EGFR E746_A750/MET amp):>3.3 μM, H1781 (ErbB2 Ins G776V, C):744 nM , PC9 GR (EGFR Del E746_A750/T790M):8 nM, PC9 (EGFR Del E746_A750):6 nM, H3255 (EGFR L858R):66 nM, Calu3 (ErbB2 amp):915 nM |
| 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] |
| Cell Research | Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference) |
| Molecular Weight | 481.01 |
| Formula | C24H25ClN6OS |
| Cas No. | 1214265-57-2 |
| Smiles | CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Sc3cccc(NC(=O)C=C)c3)n2)cc1 |
| Relative Density. | 1.37 g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 3 mg/mL (6.23 mM) DMSO: 89 mg/mL (185 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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