Pomalidomide

製品コードS1567 バッチS156705

印刷

化学情報

Chemical Structure Synonyms CC-4047 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H11N3O4
分子量 273.24 CAS No. 19171-19-8
Solubility (25°C)* 体外 DMSO 55 mg/mL (201.28 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
in vitro

Pomalidomide inhibits lipopolysaccharide (LPS) stimulated TNF-alpha release in human PBMC and in human whole blood with IC50 values of 13 nM and 25 nM, respectively. [1] Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. [2] Treatment with Pomalidomide (6.4 nM-10 μM) increases the production of IL-2 in human peripheral blood T cells, and is slightly more potent in the CD4+ subset than in the CD8+ subset. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10 levels, but only slightly more potent than CC-5013 at elevating IFN-γ levels. Pomalidomide enhances SEE and Raji cells induced AP-1 transcriptional activity in Jurkat cells in a dose-dependent manner, with a maximal enhancement of 4-fold at 1 μM. [3] Exposure of Raji cells to various concentrations of Pomalidomide (2.5-40 μg/mL) for 48 hours leads to a significant decrease in cell proliferation and DNA synthesis. There is a reduction of ~40% compared to vehicle-treated controls. [4]
in vivo

Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Administration of Pomalidomide in combination with rituximab, gives the mice a median survival period of 74 days compared with 58 days of CC5013/rituximab treatment and 45 days of rituximab nonotherapy. The synergistic effect of Pomalidomide and rituximab can be completely abrogated by depletion of NK cells, supporting the proposal that NK cell expansion is one mechanism by which Pomalidomide may augment rituximab antitumor activity. [4]
特徴 A derivative of thalidomide and up to 10,000 times more potent than thalidomide.

プロトコル(参考用のみ)

キナーゼアッセイ Inhibition of TNF-α synthesis
TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of Pomalidomide that inhibits TNF- production by 50% (IC50) is calculated by nonlinear regression analysis. The human whole blood TNF- inhibition assay is run in a similar fashion to the PBMC assay except that heparinized fresh human whole blood is plated directly into microtiter plates.
細胞アッセイ 細胞株 Raji, SU-DHL-4 and SU-DHL-10 cell lines
濃度 Dissolved in DMSO, final concentrations 2.5-40 μg/mL
反応時間 24 or 48 hours
実験の流れ

For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 μg/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL) for 24 hours or 48 hours. 1 μCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.
動物実験 動物モデル Disseminated lymphoma-bearing SCID mice
投薬量 0.5 mg/kg
投与方法 Injection i.p.

カスタマーフィードバック

Data from [Blood, 2011, 118, 4771-4779]

Data from [Data independently produced by , , Blood Cancer Journal, 2015, 5: e312]

Data from [Data independently produced by , , Haematologica, 2017, 102(12):2113-2124]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting the mSWI/SNF Complex in POU2F-POU2AF Transcription Factor-Driven Malignancies [ bioRxiv, 2024, :2024.01.22.576669.] PubMed: 38328238
BRD4-targeting PROTAC as a unique tool to study biomolecular condensates [ Cell Discov, 2023, 9(1):47] PubMed: 37156794
SUMOylation inhibition overcomes proteasome inhibitor resistance in multiple myeloma [ Blood Adv, 2023, 7(4):469-481] PubMed: 35917568
Daratumumab induces cell-mediated cytotoxicity of primary effusion lymphoma and is active against refractory disease [ Oncoimmunology, 2023, 12(1):2163784] PubMed: 36632565
CD38-Induced Metabolic Dysfunction Primes Multiple Myeloma Cells for NAD+-Lowering Agents [ Antioxidants (Basel), 2023, 12(2)494] PubMed: 36830052
Exosome-Modified Liposomes Targeted Delivery of Thalidomide to Regulate Treg Cells for Antitumor Immunotherapy [ Pharmaceutics, 2023, 15(4)1074] PubMed: 37111560
IMiD/CELMoD-induced growth suppression of adult T-cell leukemia/lymphoma cells via cereblon through downregulation of target proteins and their downstream effectors [ Front Oncol, 2023, 13:1272528] PubMed: 38344143
Novel dual LSD1/HDAC6 inhibitor for the treatment of cancer [ PLoS One, 2023, 18(1):e0279063] PubMed: 36595522
Vactosertib, a novel TGF-β1 type I receptor kinase inhibitor, improves T-cell fitness: a single-arm, phase 1b trial in relapsed/refractory multiple myeloma [ Res Sq, 2023, rs.3.rs-3112163] PubMed: 37503043
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272

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人間や獣医の診断であるか治療的な使用のためにでない。

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