WZ3146
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, J?nne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 464.95 |
| Cas No. | 1214265-56-1 |
| Formula | C24H25ClN6O2 |
| Solubility | ≥23.25 mg/mL in DMSO with gentle warming |
| Chemical Name | N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide |
| SDF | Download SDF |
| Canonical SMILES | C=CC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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 | ||||
Quality Control & MSDS
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Chemical structure
