Thalidomide

製品コードS1193 バッチS119304

印刷

化学情報

Chemical Structure Synonyms K17 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H10N2O4
分子量 258.23 CAS No. 50-35-1
Solubility (25°C)* 体外 DMSO 51 mg/mL (197.49 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 30%PEG300 1%Tween80 64%ddH2O (suspension)

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (19.36mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 10 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 640 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.
in vitro

Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite. [1] This compound selectively inhibits the production of human monocyte tumor necrosis factor alpha (TNF-alpha) when human monocytes are triggered with lipopolysaccharide and other agonists in culture. [2] It exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. [3] This chemical acts directly, by inducing apoptosis or G1 growth arrest, in MM cell lines and in patient MM cells that are resistant to melphalan, doxorubicin, and dexamethasone (Dex). It enhances the anti-MM activity of Dex and, conversely, are inhibited by interleukin 6. [4] This agent is a potent costimulator of primary human T cells in vitro, synergizing with stimulation via the T cell receptor complex to increase interleukin 2-mediated T cell proliferation and interferon gamma production. It also increases the primary CD8+ cytotoxic T cell response induced by allogeneic dendritic cells in the absence of CD4+ T cells. [5]
in vivo

Thalidomide (200 mg/kg) results in an inhibition of the area of vascularized cornea of rabbits that ranged from 30% to 51% in three experiments with a median inhibition of 36%. [1]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/7513432/
  • https://pubmed.ncbi.nlm.nih.gov/1997652/
  • https://pubmed.ncbi.nlm.nih.gov/8496685/
  • https://pubmed.ncbi.nlm.nih.gov/11049970/
  • https://pubmed.ncbi.nlm.nih.gov/9607928/
  • https://pubmed.ncbi.nlm.nih.gov/25043012/

カスタマーフィードバック

Data from [Data independently produced by , , Blood, 2017, 129(10):1308-1319]

Data from [Data independently produced by , , FASEB Journal, 2015, fj.15-274050]

Data from [Data independently produced by , , Oncotarget, 2016, 7(25):38539-38550]

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 histone H2B acetylated enhanceosomes via p300/CBP degradation in prostate cancer [ Nat Genet, 2025, 57(10):2468-2481] PubMed: 41044247
Enhancing T cell cytotoxicity in multiple myeloma with bispecific αPD-L1 × αCD3 T cell engager-armed T cells and low-dose bortezomib therapy [ Biomed Pharmacother, 2025, 184:117878] PubMed: 39891948
Stepwise phosphorylation and SUMOylation of PIDD1 drive PIDDosome assembly in response to DNA repair failure [ Nat Commun, 2024, 15(1):9195] PubMed: 39448602
Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition [ Cell Rep Med, 2024, 5(10):101752] PubMed: 39353441
A small-molecule degrader selectively inhibits the growth of ALK-rearranged lung cancer with ceritinib resistance [ iScience, 2024, 27(2):109015.] PubMed: 38327793
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
p300/CBP degradation is required to disable the active AR enhanceosome in prostate cancer [ bioRxiv, 2024, 2024.03.29.587346] PubMed: 38586029
Protocol to generate cardiac pericytes from human induced pluripotent stem cells [ STAR Protoc, 2023, 4(2):102256] PubMed: 37119139
Lenalidomide bypasses CD28 co-stimulation to reinstate PD-1 immunotherapy by activating Notch signaling [ Cell Chem Biol, 2022, S2451-9456(22)00204-5] PubMed: 35732177
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746

長期の保管のために-20°Cの下で製品を保ってください。

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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