WZ4002 - Moligand™, 10mM in DMSO , Inhibitor of BLK proto-oncogene; Src family tyrosine kinase;Inhibitor of Bruton tyrosine kinase;Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of IL2 inducible T ce, Inhibitor of BLK proto-oncogene; Src family tyrosine kinase;Inhibitor of Bruton tyrosine kinase;Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of IL2 inducible T cell kinase;Inhibitor of NUAK family
WZ4002 - Moligand™, 10mM in DMSO , Inhibitor of BLK proto-oncogene; Src family tyrosine kinase;Inhibitor of Bruton tyrosine kinase;Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of IL2 inducible T ce, Inhibitor of BLK proto-oncogene; Src family tyrosine kinase;Inhibitor of Bruton tyrosine kinase;Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of IL2 inducible T cell kinase;Inhibitor of NUAK family
GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
WZ4002 is a novel, mutant-selective EGFR inhibitor forEGFR(L858R)/(T790M)withIC50of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I). In vitro
WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and WZ4002 prevents of EGFR phosphorylation in NIH-3T3 cells expressing different EGFR T790M mutant alleles. For WZ4002, kinases that exhibited greater than 95% inhibition relative to the DMSO control at 10 μM are selected for measurement of their dissociation constants. WZ4002, which possesses an ortho-methoxy group at the C2-aniline substituent, is more selective for EGFR compared to WZ3146. WZ4002 is 100-fold less effective at inhibiting phosphorylation of WT EGFR compared to the quinazoline inhibitors. Similarly, WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib. In addition, the phosphorylated EGFR of Src TKI-resistant H1975 cells, as well as HCC827 cells, is completely suppressed by the third generation EGFR TKI, WZ4002.
In vivo
In a 2-week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Treatment with low-dose WZ4002, and high-dose WZ4002 leads to mean decreases in tracer uptake of 26%, and 36%, respectively. Cell Data
WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of BLK proto-oncogene; Src family tyrosine kinase;Inhibitor of Bruton tyrosine kinase;Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 4;Inhibitor of IL2 inducible T cell kinase;Inhibitor of NUAK family
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