WZ8040

• Catalog No.: S1179
• CAS Number: 1214265-57-2
• M. F.: C24H25ClN6OS
• M. W.: 481.0129
• Storage: -20°C

SYNONYMS

• IUPAC name: N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)sulfanyl]phenyl}prop-2-enamide
• IUPAC Traditional name: N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)sulfanyl]phenyl}prop-2-enamide

DATABASE IDS

• CAS Number: 1214265-57-2

PROPERTIES

• Target: EGFR
• Salt Data: Free Base
• Solubility: DMSO
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Cancer

Biological Activity

• Description: WZ8040 is a novel mutant-selective irreversible EGFR^T790M inhibitor.
• Targets: EGFR T790M
• 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]
• Features: Inhibits EGFR^T790M mutation but not wild-type EGFR.

Protocol

• Protocol: Cell Assay ^[1]
• Cell Lines: HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3
• Concentrations: Dissolved in DMSO, final concentrations ~10 μM
• Incubation Time: 72 hours
• Methods: Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.

References

• References: [1] Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.

REFERENCES

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