WZ8040EGFR T790M inhibitor,irreversible amd potent CAS# 1214265-57-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1214265-57-2 | SDF | Download SDF |
| PubChem ID | 44607531 | Appearance | Powder |
| Formula | C24H25ClN6OS | M.Wt | 481.01 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | WZ-8040;WZ 8040 | ||
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]sulfanylphenyl]prop-2-enamide | ||
| SMILES | CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)SC4=CC=CC(=C4)NC(=O)C=C)Cl | ||
| Standard InChIKey | KIISCIGBPUVZBF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H25ClN6OS/c1-3-22(32)27-18-5-4-6-20(15-18)33-23-21(25)16-26-24(29-23)28-17-7-9-19(10-8-17)31-13-11-30(2)12-14-31/h3-10,15-16H,1,11-14H2,2H3,(H,27,32)(H,26,28,29) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | WZ8040 is an irreversible inhibitor of EGFR T790M with IC50 value of <10nM. | |||||
| Targets | EGFR T790M | |||||
| IC50 | <10nM | |||||
WZ8040 Dilution Calculator
WZ8040 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.079 mL | 10.3948 mL | 20.7896 mL | 41.5792 mL | 51.974 mL |
| 5 mM | 0.4158 mL | 2.079 mL | 4.1579 mL | 8.3158 mL | 10.3948 mL |
| 10 mM | 0.2079 mL | 1.0395 mL | 2.079 mL | 4.1579 mL | 5.1974 mL |
| 50 mM | 0.0416 mL | 0.2079 mL | 0.4158 mL | 0.8316 mL | 1.0395 mL |
| 100 mM | 0.0208 mL | 0.1039 mL | 0.2079 mL | 0.4158 mL | 0.5197 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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WZ8040 is a novel, irreversible mutant-selective EGFR kinase inhibitor that specifically inhibits phosphorylation of EGFRT790M.
WZ8040 shows to suppress the growth of EGFR T790M containing cell lines as well as inhibit phosphorylation of EGFR in the Non–Small-Cell Lung Cancer (NSCLC) cells. WZ8040 was identified from the screen that possessed up to a 300-fold lower IC50 against the PC9GR cells compared to clinical stage inhibitors such as HKI-272 [1].
References:
[1] Zhou W1, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.
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WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.
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