生物活性
WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal[1].
体外研究
WZ8040 exhibits IC50 values of 1 nM for HCC827 (EGFR Del E746_A750), 6 nM for PC9 (EGFR Del E746_A750), 66 nM for H3255 (EGFR L858R), 9 nM for H1975 (EGFR L858R/T790M), 8 nM for PC9 GR (EGFR Del E746_A750/T790M), >3.3 μM for HCC827 GR (EGFR E746_A750/MET amp), 738 nM for H1819 (ERBB2 amp), 915 nM for Calu-3 (ERBB2 amp), 744 nM for H1781 (ERBB2 Ins G776V, C), 1.82 μM for HN11 (EGFR & ERBB2 WT), respectively[1].
Western Blot Analysis[1]
Cell Line: NSCLC cell lines and Ba/F3 cells.
Concentration: 0-3.3 μM.
Incubation Time: 24 hours.
Result: Exhibited activity for EGFR-mutated NSCLC lines, such as HH827, PC9, H3255, H1819, Calu-3, H1781 and HN11 cells.
分子量
481.01
性状
Solid
Formula
C24H25ClN6OS
CAS 号
1214265-57-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : 25 mg/mL (51.97 mM; ultrasonic and warming and heat to 60°C)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.0790 mL 10.3948 mL 20.7896 mL
5 mM 0.4158 mL 2.0790 mL 4.1579 mL
10 mM 0.2079 mL 1.0395 mL 2.0790 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: