Thalidomide

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.

CAS No. 50-35-1

サイズ	価格(税別)	在庫状況
200mg	JPY 15200	国内在庫あり
1g	JPY 43800	国内在庫なし(納期7~10日)

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Thalidomide関連製品

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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
RAW264.7	Antiinflammatory assay	10 uM	3 hrs	Antiinflammatory activity in mouse LPS-activated RAW264.7 cells assessed as ROS scavenging activity at 10 uM pretreated for 3 hrs before LPS challenge measured by decrease in fluorescent intensity by confocal microscopy	18723357
RAW264.7	Function assay	1 uM	3 hrs	Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 1 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot	18723357
RAW264.7	Function assay	10 uM	3 hrs	Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot	18723357
RAW264.7	Function assay	10 uM	3 hrs	Reduction in pERK1/2 expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot	18723357
Ehrlich ascites carcinoma cells	Toxicity assay	1.25 mM/kg	7 days	Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal degeneration of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis	18951804
Ehrlich ascites carcinoma cells	Toxicity assay	1.25 mM/kg	7 days	Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal necrosis of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis	18951804
BTI-TN-5B1-4	Function assay		30 mins	Binding affinity to human CRBN (1 to 442 residues)/N-terminal 6His-tagged human DDB1 (1 to 1140 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells after 30 mins by cy5 probe based fluorescence polarization assay, Kd=0.25μM	31117518
HeLa	Function assay			Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50=2.04μM	17845850
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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.

Targets

E3 Ligase ^[6]
(Cell-free assay)

TNF-alpha ^[2]
(Cell-free assay)

In Vitro
In vitro	Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite. ^[1] Thalidomide 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] Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. ^[3] Thalidomide 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). Thalidomide enhances the anti-MM activity of Dex and, conversely, are inhibited by interleukin 6. ^[4] Thalidomide 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. Thalidomide also increases the primary CD8+ cytotoxic T cell response induced by allogeneic dendritic cells in the absence of CD4+ T cells. ^[5]
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-p38 / p38 / Acetyl-H4		17620452
	Immunofluorescence	bFGF VCAM-1/CUL5 / NEDD8		25053990

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06146478	Completed	Transfusion-dependent Beta-Thalassemia	Blood Care Clinic\|Khyber Medical University Peshawar	January 25 2022	Phase 3
NCT04680195	Unknown status	Chronic Radiation Proctitis	Sixth Affiliated Hospital Sun Yat-sen University	December 14 2020	Phase 2
NCT04469556	Recruiting	Pancreatic Cancer Metastatic\|Pancreatic Ductal Adenocarcinoma\|Advanced Pancreatic Cancer	University Health Network Toronto\|Johns Hopkins University\|Cold Spring Harbor Laboratory\|Ontario Institute for Cancer Research\|Dana-Farber Cancer Institute\|Memorial Sloan Kettering Cancer Center\|Stand Up To Cancer	October 14 2020	Phase 2

参考
[1] D'Amato RJ, et al. Proc Natl Acad Sci U S A, 1994, 91(9), 4082-4085. [2] Sampaio EP, et al. J Exp Med, 1991, 173(3), 699-703. [3] Moreira AL, et al. J Exp Med, 1993, 177(6), 1675-1680. [4] Hideshima T, et al. Blood, 2000, 96(9), 2943-2950. [5] Haslett PA, et al. J Exp Med, 1998, 187(11), 1885-1892. [6] Eric S Fischer, et al. Nature . 2014 Aug 7;512(7512):49-53. + 展開

参考

+ 展開

化学情報

分子量	258.23	化学式	C₁₃H₁₀N₂O₄
CAS No.	50-35-1	SDF	Download Thalidomide SDFをダウンロードする
Smiles	C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 51 mg/mL ( (197.49 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

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):