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

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.98%

99.98

Relaterade mål	Proteasome E1 Activating E3 Ligase DUB SUMO p97 E2 conjugating
Övrigt E3 ligase Ligand Inhibitorer	CC-99282

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning	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
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	258.23	Formel	C₁₃H₁₀N₂O₄	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	50-35-1	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	K17			Smiles	C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O

Löslighet (Solubility)

In vitro
Batch:

DMSO : 150 mg/mL (580.87 mM) Uppvärmd med 60°C vattenbad; Ultraljudsbehandlad;
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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) Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (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%.
Referenser	[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/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	PMID
Western blot	p-p38 / p38 / Acetyl-H4		17620452
Immunofluorescence	VCAM-1/CUL5 / NEDD8 bFGF		29746508

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
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

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):

Thalidomide E3 ligase Ligand Kemikalie

Molekylvikt: 258.23

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Thalidomide E3 ligase Ligand Kemikalie

Molekylvikt: 258.23

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)