Name: Pomalidomide (CC-4047)
Brand: Selleck Chemicals
SKU: S1567
Availability: InStock
Rating: 5 (122 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 Inhibitors	CC-99282

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (365.97 mM)
(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.
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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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 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	273.24	Formula	C₁₃H₁₁N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	19171-19-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CC-4047			Smiles	C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)N

Mechanism of Action

Features	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.
Kinase Assay	Inhibition of TNF-α synthesis
Kinase Assay	TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of this compound that inhibits TNF- production by 50% (IC50) is calculated by nonlinear regression analysis. The human whole blood TNF- inhibition assay is run in a similar fashion to the PBMC assay except that heparinized fresh human whole blood is plated directly into microtiter plates.
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.
References	[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/

Applications

Methods	Biomarkers	Images	PMID
Western blot	CEBPβ IKZF1 / IKZF3 / UBE2G1 / CRBN		21389327
Immunofluorescence	IKZF1		29496670

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

Tech Support

Handling Instructions

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Frequently Asked Questions

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

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

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

Answer:
Our S1567 is racemic.

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Pomalidomide (CC-4047) Immunomodulatory agent

Chemical Structure

Molecular Weight: 273.24