Name: Pomalidomide (CC-4047)
Brand: Selleck Chemicals
SKU: S1567
Rating: 5 (123 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	Formulering	Aktivitetsbeskrivning	PMID
MOLP-8	Cytotoxicity Assay	10 μM	24 h		potently augments direct and indirect MM cell killing by SAR	26338273
J-CD38	Cytotoxicity Assay	10 μM	24 h		potently augments direct and indirect MM cell killing by SAR	26338273
R-CD38	Cytotoxicity Assay	10 μM	24 h		potently augments direct and indirect MM cell killing by SAR	26338273
BC-3	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=107 nM, inhibits cell IC50=107 nM, viability dose dependently	26119939
BCBL-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=74 nM, inhibits cell viability dose dependently	26119939
JSC-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=34 nM, inhibits cell viability dose dependently	26119939
VG-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=101 nM, inhibits cell viability dose dependently	26119939
UMPEL-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=32 nM, inhibits cell viability dose dependently	26119939
UMPEL-3	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=111 nM, inhibits cell viability dose dependently	26119939
BC-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=744 nM, inhibits cell viability dose dependently	26119939
BCP-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=396 nM, inhibits cell viability dose dependently	26119939
APK-1	Growth Inhibition Assay	39-1250 nM	5 d	DMSO	IC50=226 nM, inhibits cell viability dose dependently	26119939
RPMI8226	Growth Inhibition Assay	0.01-50 μM	48 h	DMSO	IC50=8 μM	26097872
OPM2	Growth Inhibition Assay	0.01-50 μM	48 h	DMSO	IC50=10 μM	26097872
RPMI8226	Function Assay	10 μM	48 h	DMSO	strengthens cytoplasmic-nuclear shuttling of mTOR and p-mTOR protein	26097872
OPM2	Function Assay	10 μM	48 h	DMSO	strengthens cytoplasmic-nuclear shuttling of mTOR and p-mTOR protein	26097872
RPMI8226	Function Assay	0.1-10 μM	4 h	DMSO	increases VEGF mRNA expression	25053990
SH-SY5Y	Apoptosis Assay	25 μg/mL	1 h		causes statistically significant reduction in both CPF- and CPF+CM-induced apoptosis	24975276
JJN3	Growth Inhibition Assay	0.1-100 μM	72 h	DMSO	inhibits cell growth slightly	23178378
XG-1	Growth Inhibition Assay	0.1-100 μM	72 h	DMSO	inhibits cell growth	23178378
CD138+	Growth Inhibition Assay	0.1-100 μM	72 h	DMSO	inhibits cell growth	23178378
XG-1	Function Assay	2/100 μM	24 h	DMSO	inhibits CCL3/MIP-1α mRNA expression	23178378
U266	Growth Inhibition Assay	0.01-10 μM	48 h	DMSO	inhibits cell growth dose dependently	22552008
CRBN60	Growth Inhibition Assay	0.01-10 μM	48 h	DMSO	inhibits cell growth dose dependently	22552008
CRNB75	Growth Inhibition Assay	0.01-10 μM	48 h	DMSO	inhibits cell growth dose dependently	22552008
MM.1S	Growth Inhibition Assay	0.01-10 μM	48 h	DMSO	significantly inhibits proliferation at concentrations as low as 0.01μM	21389327
OPM2	Growth Inhibition Assay	0.01-10 μM	48 h	DMSO	significantly inhibits proliferation at concentrations as low as 0.01μM	21389327
MM.1S	Function Assay	10 μM	72 h	DMSO	significantly decreases the protein level of C/EBPβ isoforms	21389327
H929	Function Assay	10 μM	72 h	DMSO	significantly decreases the protein level of C/EBPβ isoforms	21389327
OPM2	Function Assay	10 μM	72 h	DMSO	significantly decreases the protein level of C/EBPβ isoforms	21389327
CT26	Function Assay	1/10 μM	24 h		reduces the numbers of live colonies	19638977
T-cells	Function assay		2 to 3 days		Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA, EC50 = 0.008 μM.	23168019
DF15	Function assay		4 hrs		Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing ePL-tagged aiolos after 4 hrs by luminometric analysis, EC50 = 0.022 μM.	28425720
DF15	Function assay		4 hrs		Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis, EC50 = 0.024 μM.	28425720
DF15	Function assay		4 hrs		Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF15 cells expressing pLOC-ePL-tagged aiolos after 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay, EC50 = 0.027 μM.	28358507
NAMALWA	Antiproliferative assay		72 hrs		Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.03 μM.	23168019
HeLa	Function assay				Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50 = 1.27 μM.	17845850
DF15	Function assay	0.01 to 1 uM	5 hrs		Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis	28425720
OPM2	Function assay	0.01 to 1 uM	5 hrs		Induction of cereblon-mediated ikaros degradation in human OPM2 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis	28425720
DF15	Function assay	0.01 to 1 uM	5 hrs		Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis	28425720
OPM2	Function assay	0.01 to 1 uM	5 hrs		Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis	28425720
Klicka för att visa mer experimentella data för cellinjer

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

Molekylvikt	273.24	Formel	C₁₃H₁₁N₃O₄	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	19171-19-8	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	CC-4047			Smiles	C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)N

Löslighet (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (365.97 mM)
(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.
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.
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	3%DMSO 1 40%PEG300 2 5%Tween80 3 52%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	3.000mg/ml (10.98mM)	Taking the 1 mL working solution as an example, add 30 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 520 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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)

Egenskaper	A derivative of thalidomide and up to 10,000 times more potent than thalidomide.
Targets/IC₅₀/Ki	CRBN TNF-α (PBMCs) 13 nM
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. This compound inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. Treatment with this chemical (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. It 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. This agent 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. Exposure of Raji cells to various concentrations of this compound (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.
Kinasanalys	Hämning av TNF-α-syntes
Kinasanalys	TNF-α-hämmande aktivitet mäts i lipopolysackarid (LPS)-stimulerade PBMC. Pomalidomide tillsätts till humana PBMC 1 timme före tillsats av LPS (1 μg/mL) och inkubation fortsätter i ytterligare 18-20 timmar. Supernatanter skördas sedan, och koncentrationen av TNF-α i supernatanterna bestäms med ELISA. Koncentrationen av denna förening som hämmar TNF-produktion med 50% (IC50) beräknas med icke-linjär regressionsanalys. Analysen för hämning av TNF- i humant helblod utförs på ett liknande sätt som PBMC-analysen, förutom att hepariniserat färskt humant helblod pläteras direkt i mikrotiterplattor.
In vivo	Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Administration of this compound 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 this compound and rituximab can be completely abrogated by depletion of NK cells, supporting the proposal that NK cell expansion is one mechanism by which this compound may augment rituximab antitumor activity.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/10386948/ [2] https://pubmed.ncbi.nlm.nih.gov/19009291/ [3] https://pubmed.ncbi.nlm.nih.gov/12649301/ [4] https://pubmed.ncbi.nlm.nih.gov/16115943/ [5] https://pubmed.ncbi.nlm.nih.gov/26051217/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	PMID
Western blot	CEBPβ IKZF1 / IKZF3 / UBE2G1 / CRBN		21389327
Immunofluorescence	IKZF1		29496670

Klinisk prövningsinformation (Clinical Trial Information)

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

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT04902443	Recruiting	Viral Associated Malignancies\|Kaposi Sarcoma\|EBV/KSHV-associated Lymphomas	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	December 10 2021	Phase 1

Vanliga frågor (Frequently Asked Questions)

Fråga 1:
Is the formulation S1567 in 1% DMSO+30% polyethylene glycol+1% Tween 80 suitable for its oral administration?

Svar:
Its suspension in 1% DMSO+30% polyethylene glycol+1% Tween 80 is for oral gavage.

Fråga 2:
I would like to know if it is racemic or optically active?

Svar:
Our S1567 is racemic.

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):

Pomalidomide (CC-4047) Immunmodulerande medel

Molekylvikt: 273.24

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)

Vanliga frågor (Frequently Asked Questions)

Pomalidomide (CC-4047) Immunmodulerande medel

Molekylvikt: 273.24

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)

Vanliga frågor (Frequently Asked Questions)

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