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CRBN配体
凋亡 TNF-alpha 细胞凋亡诱导剂
/ Lenalidomide

来那度胺 /Lenalidomide {[allProObj[0].p_purity_real_show]}

货号：A368764 同义名： CC-5013

Lenalidomide, a analog of thalidomide, is TNF-α secretion inhibitor with IC50 of 13 nM.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lenalidomide 化学结构 CAS号：191732-72-6
Lenalidomide 化学结构
CAS号：191732-72-6
Lenalidomide 3D分子结构
CAS号：191732-72-6
Lenalidomide 化学结构 CAS号：191732-72-6
Lenalidomide 3D分子结构 CAS号：191732-72-6
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Lenalidomide 纯度/质量文件 产品仅供科研

货号：A368764 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 TNF-α ↓ 其他靶点 纯度
Thalidomide ✔ E3 Ligase 98%
GSK2982772 ++

human RIP1, IC50: 16 nM

 		99%+
QNZ ++++

TNF-α, IC50: 7 nM

 		NF-κB 99%+
Lenalidomide +++

TNF-α, IC50: 13 nM

 		98%
Pomalidomide +++

TNF-α, IC50: 13 nM

 		98%
GSK481 ✔ 99%+
Apremilast ++

TNF-α, IC50: 77 nM

 		98%
Necrostatin-1 +

RIP1, EC50: 490 nM

 		99%+
Acetylcysteine ✔ 98%
Adalimumab ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lenalidomide 生物活性

靶点

  • TNF-α

    TNF-α, IC50:13 nM

  • CRBN
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].

Lenalidomide 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
A388 Growth Inhibition Assay IC50=60.449 μM SANGER

Lenalidomide 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 <<

Lenalidomide 参考文献

[1]343(6168):305-9.

[2]343(6168):305-9.

[3]Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG Jr. The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science. 2014 Jan 17;343(6168):305-9.

[4]Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG Jr. The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science. 2014 Jan 17;343(6168):305-9.

Lenalidomide 实验方案

计算器
存储液制备 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

Lenalidomide 技术信息

CAS号191732-72-6
分子式C13H13N3O3
分子量 259.261
别名 CC-5013
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
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
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

Tags: Lenalidomide | CC-5013 | Apoptosis Inducer | Apoptosis | TNF-alpha | CRBN Ligand | AmBeed-信号通路专用抑制剂 | Lenalidomide 纯度/质量文件 | Lenalidomide 亚型比较 | Lenalidomide 生物活性 | Lenalidomide 细胞研究 | Lenalidomide 临床数据 | Lenalidomide 参考文献 | Lenalidomide 实验方案 | Lenalidomide 技术信息

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