ホームページ Ubiquitin E3 ligase Ligand chemical - TNF-alpha inhibitor - E3 Ligase inhibitor - VEGFR inhibitor - Caspase activator - Apoptosis related activator Lenalidomide For research use only.

Lenalidomide

別名：CC-5013

Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) 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 promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

Lenalidomide化学構造

CAS No. 191732-72-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 28600 国内在庫あり
JPY 22000 国内在庫あり
JPY 44500 国内在庫あり
JPY 100500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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製品安全説明書

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Lenalidomide関連製品

E3 ligase Ligand阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
DF15 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
OPM2 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
DF15 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
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生物活性

製品説明 Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) 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 promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Targets
CRBN [3] VEGF [1] TNF-α [1]
(PBMCs)
13 nM
In Vitro
In vitro

Lenalidomide strongly induces IL-2 and sIL-2R production. Lenalidomide-induced tyrosine phosphorylation of CD28 on T cells is followed by a down-stream activation of NF-κB. [2]

Lenalidomide and pomalidomide inhibits autoubiquitination of CRBN in HEK293 T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA). Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for Lenalidomide resistance in H929 myeloma cell lines is accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and Lenalidomide, CRBN protein is undetectable. [3]

Lenalidomide prevents induction of defects by down-regulating tumor cell inhibitory molecule expression. Lenalidomide prevents induction of tumor-induced T cell lytic synapse dysfunction. Lenalidomide treatment blocks CLL cell-induced T cell actin synapse dysfunction, mimicks antibody blockade, and down-regulates expression of CLL inhibitory ligands and their receptors on T cells. Lenalidomide treatment prevents tumor-induced immune suppression in FL, DLBCL, HL, MM, SCC, and OC and down-regulates immunosuppressive ligand expression on all tumor cells examined. CTL killing function significantly increases following antibody blockade of CLL inhibitory ligands or Lenalidomide treatment compared to control treatments. Treatment of autologous CLL-T cell co-cultures with Lenalidomide reverses impaired CD8+ T cell lytic synapse formation and granzyme B trafficking. [4]
Kinase Assay Assay for inhibition of TNF synthesis by human PBMCs
Human PBMCs from normal donors are obtained by Ficoll−Hypaque density centrifugation. Cells (106 cells/mL) are cultured in RPMI supplemented with 10 AB+ serum, 2 mM l-glutamine, 100 U/mL penicillin, and 100 μg/mL streptomycin. Lenalidomide is dissolved in DMSO at 20 mg/mL; further dilution is done with culture medium. The final DMSO concentration in all assays including the controls is 0.25%. Lenalidomide is added to cells 1 hour prior to the addition of LPS. PBMCs (106 cells/mL) are stimulated with 1 μg/mL of LPS from Salmonella minnesota R595. Cells, in triplicate, are incubated with LPS for 18−20 hours at 37 °C in 5% CO2. Supernatants are then harvested and assayed for cytokine levels. In some experiments, supernatants are kept frozen at −70 °C until use. Cell viability is assayed by Trypan blue exclusion dye method. The concentration of TNFα in the culture supernatants is determined by ELISA. Lenalidomide is assayed in a minimum of three separate experiments. Percent inhibition is determined as 100 × [1 − (cytokine(experimental)/cytokine(control))].
実験結果図 Methods Biomarkers 結果図 PMID
Western blot MDM2 / p-MDM2 / p-p53 / p53 phospho-IKKβ / IKKβ 22525275
Growth inhibition assay Cell viability 22698399
In Vivo
In Vivo

The induction of angiogenesis by bFGF is significantly inhibited by oral treatment of Lenalidomide in a dose-dependent manner. Lenalidomide significantly decreases the percentage of vascularized area from 5.16% (control group) to 2.58% (50 mg/kg). Lenalidomide significantly reduces the calculated total MVL from 21.07 (control) to 8.11 (50 mg/kg). Lenalidomide significantly inhibites HUVEC migration through the fibronectin-coated membranes towards 0.1 ng/mL of bFGF at 100 μM, 1 ng/mL of VEGF at concentrations of 10 μM and 100 μM. [5]
動物実験 動物モデル Adult male Sprague-Dawley rats bearing HUVECs cells
投与量 50 mg/kg and 250 mg/kg
投与経路 Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06177028 Not yet recruiting
Cognitive Impairment Mild|Cognitive Dysfunction|Amyloid Plaque|Neurodegenerative Disease Hereditary|Inflammation Brain
St. Joseph''s Hospital and Medical Center Phoenix|Texas Tech University
 January 2 2024 Phase 2
NCT06149286 Recruiting
Relapsed/Refractory Follicular Lymphoma|Marginal Zone Lymphoma (MZL)
Regeneron Pharmaceuticals
 December 28 2023 Phase 3
NCT06299553 Recruiting
DLBCL - Diffuse Large B Cell Lymphoma
Incyte Biosciences Italy S.r.l
 December 4 2023 --

化学情報

分子量 259.26 化学式

C13H13N3O3
CAS No. 191732-72-6 SDF Download Lenalidomide SDFをダウンロードする
Smiles C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N
保管

In vitro
Batch:

DMSO : 52 mg/mL ( (200.57 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機
Clear solution
5%DMSO 40% 5% 50%ddH2O
10.0mg/ml (38.57mM) Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
What is the formulation for mouse injection(i.p.)?

回答
This paper has the information you need: http://link.springer.com/article/10.1208/s12248-012-9401-2. Add lenalidomide to the appropriate volume of sterile phosphate-buffered saline (PBS) containing 1% hydrochloric acid (HCl). the pH of this preparation was adjusted to 7.0–7.6 using sodium hydroxide and sterile filtered using a 0.22 μm Steriflip filter.

質問2:
what is the procedure to resuspend this compound？

回答
You can resuspend this compund by DMSO, the solubility is about 52 mg/mL (200.57 mM). For in vivo study, you can prepare the working solution with the vehicle of: 30% PEG400/0.5% Tween80/5% propylene glycol for oral administration.

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