WZ3146Mutant EGFR inhibitor, potent and irreversible CAS# 1214265-56-1 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1214265-56-1 | SDF | Download SDF |
| PubChem ID | 44607360 | Appearance | Powder |
| Formula | C24H25ClN6O2 | M.Wt | 464.95 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 150 mg/mL (322.62 mM; Need ultrasonic) | ||
| Chemical Name | N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide | ||
| SMILES | CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl | ||
| Standard InChIKey | APHGZZPEOCCYNO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H25ClN6O2/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 | WZ3146 is a potent and irreversible inhibitor of mutant EGFR with IC50 values of both 2 nM for EGFR(L858R) and EGFR(E746_A750). | |||||
| Targets | EGFR(L858R) | EGFR(E746_A750) | ||||
| IC50 | 2 nM | 2 nM | ||||
WZ3146 Dilution Calculator
WZ3146 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1508 mL | 10.7538 mL | 21.5077 mL | 43.0154 mL | 53.7692 mL |
| 5 mM | 0.4302 mL | 2.1508 mL | 4.3015 mL | 8.6031 mL | 10.7538 mL |
| 10 mM | 0.2151 mL | 1.0754 mL | 2.1508 mL | 4.3015 mL | 5.3769 mL |
| 50 mM | 0.043 mL | 0.2151 mL | 0.4302 mL | 0.8603 mL | 1.0754 mL |
| 100 mM | 0.0215 mL | 0.1075 mL | 0.2151 mL | 0.4302 mL | 0.5377 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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WZ3146 is a novel, irreversible inhibitor that specifically inhibits phosphorylation of EGFR(L858R0) and EGFR(E746_A750) with IC50 values of 2nM each.
WZ3146 has been reported to inhibit the phosphorylation of EGFR in the Non–Small-Cell Lung Cancer (NSCLC) cell lines [1]. WZ3146 shows to suppress the growth of EGFR T790M containing cell lines. Besides, Analysis of recombinant EGFR T790M kinase incubated with WZ3146 by electrospray mass spectrometry revealed stoichiometric addition of one inhibitor molecule to the protein. Analysis of a pepsin digest of the modified protein by tandem MS identified Cys 797 as the site of modification thus verifying covalent bond formation between WZ3146 and EGFR [2].
References:
[1] Thanyanan Reungwetwattana, Saravut J. Weroha, Julian R. Molina. Oncogenic Pathways, Molecularly Targeted Therapies, and Highlighted Clinical Trials in Non–Small-Cell Lung Cancer (NSCLC). Clinical Lung Cancer, Volume 13, Issue 4, July 2012, Pages 252-266
[2] 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.
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