生物活性 | |||
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描述 | A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity; completely and selectively depletes BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation; displays strong growth inhibition and apoptosis induction activity in TNBC cell lines with IC50 <1 uM, induces a rapid and time-dependent downregulation of MCL1 protein; decreases BET proteins in xenograft breast tumors and suppress tumor growth in vivo without causing weight loss. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.06mL 0.21mL 0.11mL |
5.29mL 1.06mL 0.53mL |
10.57mL 2.11mL 1.06mL |