Lenalidomide-Br
(Synonyms: 3-(4-溴-1-氧代异吲哚啉-2-基)哌啶-2,6-二酮) 目录号 : GC38579
Lenalidomide-Br (Compound 41) 是一种基于 Lenalidomide 的 E3 泛素连接酶配体。Lenalidomide-Br 可通过 linker 与靶蛋白配体连接，形成 PROTAC 分子，PROTAC 可诱导促癌蛋白发生泛素化降解。
Cas No.:2093387-36-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lenalidomide-Br (Compound 41) is the Lenalidomide-based ligand. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
[1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17. [2]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
| Cas No. | 2093387-36-9 | SDF | |
| 别名 | 3-(4-溴-1-氧代异吲哚啉-2-基)哌啶-2,6-二酮 | ||
| Canonical SMILES | O=C(C(N(CC1=C2C=CC=C1Br)C2=O)CC3)NC3=O | ||
| 分子式 | C13H11BrN2O3 | 分子量 | 323.14 |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0946 mL | 15.4732 mL | 30.9463 mL |
| 5 mM | 0.6189 mL | 3.0946 mL | 6.1893 mL |
| 10 mM | 0.3095 mL | 1.5473 mL | 3.0946 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。
Phase 1 study of lenalidomide, bendamustine, and rituximab in previously untreated patients with chronic lymphocytic leukemia
Leuk Lymphoma 2019 Dec;60(12):2931-2938.PMID:31074316DOI:10.1080/10428194.2019.1608533
Bendamustine-rituximab (BR) is a standard therapy in CLL, and lenalidomide has single-agent activity. This phase 1 study evaluated Lenalidomide-Br as initial CLL therapy. Thirteen patients were treated at three dose levels (DL), and an additional 10 were treated at the MTD. The MTD was DL3: lenalidomide 5 mg daily D8-21 of C1, then 10 mg D1-21 of C2-6. One DLT occurred at DL2 (pulmonary embolus). Grade ≥3 toxicities included neutropenia (52.2%), rash (26.1%), anemia (21.7%), thrombocytopenia (21.7%), and febrile neutropenia (13.0%). Of 13, 9 treated at the MTD required dose modification, most for neutropenia (5). OR and CR rates were 87% and 39%, respectively. Lenalidomide-Br could be safely administered and was active as initial CLL therapy, although frequent dose modification at the MTD suggests that lenalidomide 10 mg is too high for most patients. Given the current treatment landscape, lenalidomide combinations warrant evaluation in CLL patients who are chemonaïve but have been failed by the approved targeted therapies.