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dTRIM24

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Chemical Structure| 2170695-14-2 同义名 : -
CAS号 : 2170695-14-2
货号 : A449341
分子式 : C55H68N8O13S2
纯度 : 98%
分子量 : 1113.304
MDL号 : MFCD31692370
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(94.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.90mL

0.18mL

0.09mL

4.49mL

0.90mL

0.45mL

8.98mL

1.80mL

0.90mL
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.