TD-428
目录号 : GC34319
TD-428是一种高度特异的BRD4降解剂，DC50为0.32nM。
Cas No.:2334525-50-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM[1].
TD-428, the BRD4 degrader with TD-106, is highly specific for BET proteins. TD-428 (0.01, 0.1, 1, 10, 100, 1000, and 10000 nM; 72?hours) inhibits the proliferation of 22RV1 cells with a CC50?of??20.1?nM[1].|| Cell Cytotoxicity Assay[1]|| Cell Line:|22RV1 cells|Concentration:|0.01, 0.1, 1, 10, 100, 1000, and 10000 nM|Incubation Time:|72?hours|Result:|Inhibited cell proliferation with a CC50?of?20.1?nM.|| Western Blot Analysis[1]||Cell Line:|U266 cells |Concentration:|1 nM, 10 nM, 100nM, 1000 nM, and 10?μM|Incubation Time:|12?hours|Result:|Induced the degradation of BET proteins.
[1]. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.
| Cas No. | 2334525-50-5 | SDF | |
| Canonical SMILES | O=C(NC1=CC(OCCOCCOCCNC2=C3C(N=NN(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)=CC=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5 | ||
| 分子式 | C43H43ClN10O7S | 分子量 | 879.38 |
| 溶解度 | Soluble in DMSO | 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 | 1.1372 mL | 5.6858 mL | 11.3716 mL |
| 5 mM | 0.2274 mL | 1.1372 mL | 2.2743 mL |
| 10 mM | 0.1137 mL | 0.5686 mL | 1.1372 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。
A novel cereblon modulator for targeted protein degradation
Eur J Med Chem 2019 Mar 15;166:65-74.PMID:30684871DOI:10.1016/j.ejmech.2019.01.023
Immunomodulatory drugs (IMiDs) exert anti-myeloma activity by binding to the protein cereblon (CRBN) and subsequently degrading IKZF1/3. Recently, their ability to recruit E3 ubiquitin ligase has been used in the proteolysis targeting chimera (PROTAC) technology. Herein, we design and synthesize a novel IMiD analog TD-106 that induces the degradation of IKZF1/3 and inhibits the proliferation of multiple myeloma cells in vitro as well as in vivo. Moreover, we demonstrate that TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1. Consequently, cell proliferation is inhibited due to suppressed C-MYC transcription. These results, therefore, firmly suggest that the newly synthesized IMiD analog, TD-106, is a novel CRBN modulator that can be used for targeted protein degradation.