|(2S,4R)-1-((S)-15-(叔丁基)-1-(3-(N-(1,3-二甲基-2-氧代-6-(3-丙氧基苯氧基)-2,3-二氢-1H-苯并[d]咪唑-5-基)氨磺酰基)苯基)-1,13-二氧代-5,8,11-三氧杂-2,14-二氮杂十六烷-16-酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺|CsnPharm

CAS No.: 2170695-14-2

dTRIM24 Catalog No. CSN22285

dTRIM24 is a potent and selective PROTAC targeting on TRIM24 which has been posited as a dependency in numerous cancers, with TRIM24 ligand IACS-9571 conjugated to a VHL ligand.

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400-920-2911

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技术信息

生物活性

描述dTRIM24 is a potent and selective PROTAC targeting on TRIM24 which has been posited as a dependency in numerous cancers, with TRIM24 ligand IACS-9571 conjugated to a VHL ligand. Treatment with dTRIM24 led to a max degradation of TRIM24 by 72% at concentration of 5μM in 293FT cells post 24h. A prolonged treatment with 5μM dTRIM24 for 48h degrade TRIM24 by 76% in 293FT cells. The two factors, time and concentration, exhibited interaction effect on the function of dTRIM24. dTRIM24 at concentration of 5μM possessing the max degradation of TRIM24 by 72% but almost not effect at concentration of 10μM post 24h in MOLM-13 cells, and a degradation of TRIM24 by 89% could be achieved by dTRIM24 at concentration of 2.5μM post 48h in the same cell line. dTRIM24 at concentration of 5μM inhibited MOLM-13cell proliferation within 7 days, with apoptosis shown by cleaved PARP observed at 48h^[1].
参考文献

[1] Gechijian LN, Buckley DL, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.8982 mL
- 4.4912 mL
- 8.9823 mL
- 5 mM
- 0.1796 mL
- 0.8982 mL
- 1.7965 mL
- 10 mM
- 0.0898 mL
- 0.4491 mL
- 0.8982 mL

技术信息

CAS号	2170695-14-2	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C55H68N8O13S2	运输	蓝冰
分子量	1113.30	别名

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