dTRIM24
目录号 : GC35904
dTRIM24 是一种选择性的双功能基于 PROTAC 技术的 TRIM24 降解剂。
Cas No.:2170695-14-2
Sample solution is provided at 25 µL, 10mM.
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dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC. TRIM24[2].
dTRIM24 is a degrader of TRIM24 bromodomain. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. The anti-proliferative consequences of chemical degradation versus inhibition of TRIM24 are assessed. Growth over time is determined for MOLM-13 cells treated with dTRIM24, IACS-9571, VL-269, and eTRIM24. dTRIM24 suppresses growth to a greater extent than does IACS-9571, accompanied by apoptosis measured as enhanced PARP cleavage. In agreement with a sustained proliferative defect observed following dTRIM24 treatment, near-complete degradation of TRIM24 is observed in dTRIM24-treated cells throughout the duration of the experiment[2].
[1]. Gechijian LN, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412.
Cell experiment: | MOLM-13 cells are seeded at 30,000 cells/well. Growth over time of MOLM-13 cells treated with 5?μM of indicated compounds (e.g., dTRIM24) over 7 d. At endpoints, cells are suspended and mixed with Viacount reagent at 1:3. The mixture is incubated for 5?min, and viable cells are counted on the Guava easycyte flow cytometer. Means from three technical replicates of cell counts are calculated[2]. |
References: [1]. Gechijian LN, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412. | |
| Cas No. | 2170695-14-2 | SDF | |
| Canonical SMILES | CN(C(N1C)=O)C2=C1C=C(OC3=CC=CC(OCCC)=C3)C(NS(C4=CC(C(NCCOCCOCCOCC(N[C@H](C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)C(C)(C)C)=O)=O)=CC=C4)(=O)=O)=C2 | ||
| 分子式 | C55H68N8O13S2 | 分子量 | 1113.3 |
| 溶解度 | Ethanol: < 1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet