TD-428

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Chemical Structure| 2334525-50-5 同义名 : -
CAS号 : 2334525-50-5
货号 : A1148711
分子式 : C43H43ClN10O7S
纯度 : 98%
分子量 : 879.382
MDL号 : N/A
存储条件:

Pure form

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 TD-428 is a PROTAC targeting on pan-BET with DC50 of 0.32nM for BRD4, consist of BET inhibitor, JQ1, as a warhead linked to CRBN modulator TD-106 as the E3 ligase ligand. Treatment with TD-428 for24h achieved degradation of BRD4 by78% at concentration of 0.1nM and an almost complete depletion of BRD4 at concentration>1nM, in 22RV1 cells. Further study showed that TD-428 could degrade all the BET proteins. TD-428 exhibited cytotoxicity against 22Rv1 cell line with CC50 of 20.1nM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.69mL

1.14mL

0.57mL

11.37mL

2.27mL

1.14mL

参考文献

[1]Kim SA, Go A, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.