dBET1
(Synonyms: 2-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)-N-(4-(2-((2-(2,6-二氧代哌啶-3-基)-1,3-二氧代异吲哚啉-4-基)氧基)乙酰氨基)丁基)乙酰胺) 目录号 : GC19119
A hybrid molecule containing (+)-JQ-1 and thalidomide
Cas No.:1799711-21-9
Sample solution is provided at 25 µL, 10mM.
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dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 uM, compare to IC50= 1.1 uM with JQ1)[1].
Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count[1].
References:
[1]. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81.
| Cas No. | 1799711-21-9 | SDF | |
| 别名 | 2-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)-N-(4-(2-((2-(2,6-二氧代哌啶-3-基)-1,3-二氧代异吲哚啉-4-基)氧基)乙酰氨基)丁基)乙酰胺 | ||
| Canonical SMILES | O=C(NCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4 | ||
| 分子式 | C38H37ClN8O7S | 分子量 | 785.27 |
| 溶解度 | DMSO : ≥ 50 mg/mL (63.67 mM);Water : < 0.1 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 | 1.2734 mL | 6.3672 mL | 12.7345 mL |
| 5 mM | 0.2547 mL | 1.2734 mL | 2.5469 mL |
| 10 mM | 0.1273 mL | 0.6367 mL | 1.2734 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet