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Chemical Structure : WZ4002
CAS No.: 1213269-23-8
Catalog No.: PC-42841Not For Human Use, Lab Use Only.
WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg (Free Sample) | $28 | In stock | |
| 25 mg | $128 | In stock | |
| 50 mg | $198 | In stock | |
| 100 mg | Get quote |
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WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.
WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles.
WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR.
WZ4002 suppresses the growth of erlotinib-resistant tumors caused by gatekeeper T790M mutation combined with Met kinase inhibitor E-7050 in vivo.
| M.Wt | 494.9733 | |
| Formula | C25H27ClN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Propenamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]- |
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1. Sakuma Y, et al. Lab Invest. 2012 Mar;92(3):371-83.
2. Zhou W, et al. Nature. 2009 Dec 24;462(7276):1070-4.
3. Nakagawa T, et al. Mol Cancer Ther. 2012 Oct;11(10):2149-57.
4. Ercan D, et al. Cancer Discov. 2012 Oct;2(10):934-47.
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