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  3. Ligands for E3 Ligase Molecular Glues
  4. Lenalidomide hydrochloride

Lenalidomide hydrochloride  (Synonyms: 来那度胺盐酸盐; CC-5013 hydrochloride)

目录号: HY-A0003A
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摩尔计算器

Lenalidomide hydrochloride (CC-5013 hydrochloride) 是 Thalidomide 的衍生物，也是一种具有口服活性免疫调节剂，以分子胶的方式作用。Lenalidomide hydrochloride (CC-5013 hydrochloride) 是一种泛素 E3 连接酶 cereblon (CRBN) 的配体，通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。Lenalidomide hydrochloride (CC-5013 hydrochloride) 特别地抑制成熟 B 细胞淋巴瘤 (包括多发性骨髓瘤) 的生长，并诱导 T 细胞释放白细胞介素-2 (IL-2)。

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Lenalidomide hydrochloride Chemical Structure

Lenalidomide hydrochloride Chemical Structure

CAS No. : 1243329-97-6

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Lenalidomide hydrochloride 的其他形式现货产品:

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Lenalidomide hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 32 篇科研文献

WB

    Lenalidomide hydrochloride purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):171-185.e25.  [Abstract]

    WB analysis of MV4-11 cells treated for 6.5 hr with Lenalidomide, BTX161, A51, or A86 at the indicated concentrations or DMSO.

    Lenalidomide hydrochloride purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Lenalidomide hydrochloride purchased from MCE. Usage Cited in: Oncol Rep. 2018 Jun;39(6):2873-2880.  [Abstract]

    Representative western blot membranes showing the expression levels of NF-κB p-p65 and H3 in nuclear protein and of NF-κB p65 and β-actin in total protein. β-actin and H3 are used as internal controls.

    Lenalidomide hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2017 May 22;8:15398.  [Abstract]

    HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6 h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting.

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    von Hippel-Lindau (VHL) MDM2 Cereblon IAP

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

    IC50 & Target[5]

    Cereblon

     

    体外研究
    (In Vitro)

    Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells[2]. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM[3]. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Lenalidomide hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    295.72

    Formula

    C13H14ClN3O3
    CAS 号
    中文名称

    来那度胺盐酸盐； 雷那度胺盐酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    Cell Assay
    [3]

    Cell lines NCI-H929 and U266, and DF15 cells are grown in RPMI-I640 medium containing 10% (V/V) heat-inactivated fetal bovine serum supplemented with 2 mM glutamine. To produce Lenalidomide resistant cell lines, NCI-H929 cells are treated continuously (fresh Lenalidomide is added every 3-4 days) with control (final 0.1% DMSO) or low-dose Lenalidomide (1 μM) for 2 months until the proliferation of cells is no longer inhibited by Lenalidomide (1 μM), as determined by cell viability (Vi-cell XR cell viability analyzer), cell proliferation by flow cytometry and cell cycle analysis (propidium iodide staining). After acquisition of resistance to 1 μM, the resistant H929 cell lines are treated with Lenalidomide (10 μM) for a further 4 months. After this period of time, the cell cultures achieved fully establish resistance up to high-dose Lenalidomide (30 μM). Prior to the experiments described here, H929 Lenalidomide-resistant cells are taken out of culture with compounds for 5-7 days before use[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    Imprinting control region (ICR) mice 8-10 weeks of age are used. Lenalidomide is incompletely soluble at 3.5 mg/mL and above in PBS containing 1% HCl, as visible particulates remained after thorough mixing. Therefore 3 mg/mL is selected as the maximum dosing solution concentration (with no visible particulates). Single, individual mice are initially dosed with 3, 10, or 15 mg/kg IV; 4.5, 15, or 22.5 mg/kg IP; and 9, 30, or 45 mg/kg PO. Additional mice (n=4) are then evaluated at the maximum dose achievable by volume and solubility of Lenalidomide in the dosing solution. All mice are monitored closely for 1 h and re-evaluated for toxicities 3, 6, and 24 h postdose.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Lenalidomide hydrochloride 相关分类

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    • Do most proteins show cross-species activity?

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    Keywords:

    Lenalidomide1243329-97-6CC-5013来那度胺盐酸盐 雷那度胺盐酸盐CC5013CC 5013Ligands for E3 LigaseMolecular GluesE3 ligase-recruiting MoietydegradationIKZF1IKZF3multiplemyelomaanalogimmunomodulatoryE3ligasecereblonCRL4ligandInhibitorinhibitorinhibit

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