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WZ8040

Catalog No. T6734 CAS 1214265-57-2

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

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WZ8040, CAS 1214265-57-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
5 mg	In stock	$ 95.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 259.00
50 mg	In stock	$ 385.00
100 mg	In stock	$ 567.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 98%

Biological Description

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Description	WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
Targets&IC50	Calu3 (ErbB2 amp):915 nM , H3255 (EGFR L858R):66 nM, H1975 (EGFR L858R/T790M):9 nM, HCC827 GR (EGFR E746_A750/MET amp):>3.3 μM, H1781 (ErbB2 Ins G776V, C):744 nM , PC9 (EGFR Del E746_A750):6 nM, PC9 GR (EGFR Del E746_A750/T790M):8 nM, H1819 (ErbB2 amp):738 nM , HCC827 (EGFR Del E746_A750):1 nM
In vitro	WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. [1]
Cell Research	Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference)

Molecular Weight	481.01
Formula	C24H25ClN6OS
CAS No.	1214265-57-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 3 mg/mL (6.23 mM)

DMSO: 89 mg/mL (185 mM)

References and Literature

1. Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Membrane Protein-targeted Compound Library Anti-Colorectal Cancer Compound Library Covalent Inhibitor Library Cytokine Inhibitor Library Anti-Liver Cancer Compound Library Anti-Prostate Cancer Compound Library

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Keywords

WZ8040 1214265-57-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 mutated Inhibitor phosphorylation WZ 8040 NSCLC Epidermal growth factor receptor inhibit WZ-8040 ErbB-1 inhibitor

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