WZ8040

• 产品号: S1179
• CAS号: 1214265-57-2
• 分子式: C24H25ClN6OS
• 分子量: 481.0129
• 保 存: -20°C

产品别名

• 标题: WZ8040
• IUPAC标准名: N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)sulfanyl]phenyl}prop-2-enamide
• IUPAC传统名: N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)sulfanyl]phenyl}prop-2-enamide

产品登记号

• CAS号: 1214265-57-2

产品性质

• 作用靶点: EGFR
• 成盐信息: Free Base
• 溶解度: DMSO
• 保存条件: -20°C

产品详细信息

详细说明 (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.

参考文献

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