Name: Thalidomide
Brand: Selleck Chemicals
SKU: S1193
Availability: InStock
Rating: 5 (38 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Proteasome E1 Activating E3 Ligase DUB p97 SUMO E2 conjugating
Other E3 ligase Ligand Products	CC-99282

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 150 mg/mL (580.87 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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 1 30%PEG300 2 1%Tween80 3 64%ddH2O (suspension) Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.
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.
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	258.23	Formula	C₁₃H₁₀N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	50-35-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	K17			Smiles	C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O

Mechanism of Action

Targets/IC₅₀/Ki	E3 Ligase (Cell-free assay) TNF-alpha (Cell-free assay)
In vitro	Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite. 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. It exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. 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. 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.
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%.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7513432/ [2] https://pubmed.ncbi.nlm.nih.gov/1997652/ [3] https://pubmed.ncbi.nlm.nih.gov/8496685/ [4] https://pubmed.ncbi.nlm.nih.gov/11049970/ [5] https://pubmed.ncbi.nlm.nih.gov/9607928/ [6] https://pubmed.ncbi.nlm.nih.gov/25043012/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-p38 / p38 / Acetyl-H4		17620452
Immunofluorescence	bFGF VCAM-1/CUL5 / NEDD8		25053990

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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	Active not 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

Tech Support

Handling Instructions

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Thalidomide E3 ligase Ligand chemical

Chemical Structure

Molecular Weight: 258.23