产品说明书
Lenalidomide
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同义名 : | CC-5013 |
| CAS号 : | 191732-72-6 | |
| 货号 : | A368764 | |
| 分子式 : | C13H13N3O3 | |
| 纯度 : | 98% | |
| 分子量 : | 259.261 | |
| MDL号 : | MFCD07772307 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(405 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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 9 mg/mL clear PO 0.5% CMC-Na 40 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Cereblon, encoded by CRBN gene, is the substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins. Cereblon, or the E3 ligase complex mediated normal degradation of key regulatory proteins is required for normal limb outgrowth and expression of the fibroblast growth factor FGF8. They may play a role in memory and learning by regulating the assembly and neuronal surface expression of large-conductance calcium-activated potassium channels in brain regions involved in memory and learning via its interaction with KCNT1. It was well reported that binding of thalidomide-related drugs, such as Lenalidomide, changed the substrate specificity of the E3 ligase complex, leading to decreased degradation of MEIS2 and other target proteins and increased degradation of MYC, IRF4, IKZF1 and IKZF3[3]. Lenalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. The cellular target of lenalidomide is cereblon. Another experiment revealed that Lenalidomide down regulated IKZF1 and IKZF3 and this was cereblon-dependent[4]. Lenalidomide treatment for 4 days was toxic to most ABC DLBCL cell lines[5]. 2 μM Lenalidomide led to down regulation of IKZF1, IKZF3 and IRF4 in MM1S, KMS34 and RPMI8226 cells[3]. In a MM1S xenograft model in CB17-SCID mice, Lenalidomide was administrated at the dose of 15 mg/kg i.p. 5days weekly as a single agent or in combination. The results were Lenalidomide was marginally effective as a single agent and the combination of Lenalidomide with dexamethasone or the triple combination of Lenalidomide, dexamethasone and panobinostat[6]. In an OCI-Ly10 xenograft model, daily i.p. treatment with lenalidomide at the dose of 10 mg/kg for 20 days resulted in little effect as a single agent but effective in combination with ibrutinib[5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 697 | Growth Inhibition Assay | IC50=50.3545 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=13.8199 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=35.3601 μM | SANGER | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01002703 | Multiple Myeloma | Phase 1 Phase 2 | Unknown | October 2014 | Germany ... 展开 >> University of Leipzig Recruiting Leipzig, Germany, 04103 Contact: Dietger Niederwieser +4934197 ext 13050 dietger@medizin.uni-leipzig.de Sub-Investigator: Wolfram Pönisch 收起 << |
| NCT01718743 | Myeloma | Phase 2 | Active, not recruiting | December 2020 | United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 << |
| NCT00923234 | Myelodysplastic Syndromes ... 展开 >> Acute Myelogenous Leukemia 收起 << | Phase 1 | Terminated(The primary objecti... 展开 >>ve has already been answered with the number of recruited patients.) 收起 << | - | Germany ... 展开 >> Medizinische Klinik und Poliklinik I, Uniklinik Dresden, Germany Universitätsklinikum Düsseldorf, Klinik für Hämatologie/Onkologie/klinische Immunologie Düsseldorf, Germany, 40225 Klinikum der J.W. Goethe-Universität, Medizinische Klink II Frankfurt, Germany, 60590 Technische Universität München, Klinikum Rechts der Isar München, Germany, 81675 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.86mL 0.77mL 0.39mL |
19.29mL 3.86mL 1.93mL |
38.57mL 7.71mL 3.86mL |
| 参考文献 |
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