Pomalidomide (Synonyms: CC-4047)

Name: Pomalidomide
Brand: MedChemExpress
SKU: HY-10984
Rating: 5.0 (18 reviews)

Cat. No.: HY-10984 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

For research use only. We do not sell to patients.

Pomalidomide Chemical Structure

CAS No. : 19171-19-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 154	In-stock	Estimated Time of Arrival: December 31
1 g	USD 198	In-stock	Estimated Time of Arrival: December 31
5 g	USD 495	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Pomalidomide:

16 Publications Citing Use of MCE Pomalidomide

: Pomalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430. [Abstract]; H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

: Pomalidomide purchased from MedChemExpress. Usage Cited in: Gen Comp Endocrinol. 2015 Dec 30;228:1-8. [Abstract]; TNFα significantly inhibits the mRNA and protein expression of GSK-3β, while POM significantly induces the mRNA and protein expression of GSK-3β (A). The mRNA and protein expression of β-catenin is significantly induced by TNFα, but significantly inhibited by POM (B). The protein expression of PPARγ and C/EBPα is significantly inhibited by TNFα, while significantly induced by POM treatment (C and D).

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[5]

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	> 10 μM Compound: POM	Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
B16-F10	IC₅₀	> 10 μM Compound: POM	Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
BXPC-3	IC₅₀	≤ 30 μM Compound: POM	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
JeKo-1	IC₅₀	> 20000 nM Compound: Pomalidomide	Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
JeKo-1	IC₅₀	2617.33 nM Compound: Pomalidomide	Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
K562	IC₅₀	> 10 μM Compound: Pomalidomide	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay	[PMID: 36306539]
K562	IC₅₀	> 10 μM Compound: Pomalidomide	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34217059]
KARPAS-299	IC₅₀	> 10 μM Compound: pomalidomide	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34176264]
MCF7	IC₅₀	> 100 μM Compound: Pomalidomide	Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 34864330]
MDA-MB-231	IC₅₀	> 100 μM Compound: Pomalidomide	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 34864330]
MIA PaCa-2	IC₅₀	≤ 30 μM Compound: POM	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
MM1.S	IC₅₀	21.93 nM Compound: Pomalidomide	Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
MM1.S	IC₅₀	837.8 nM Compound: Pomalidomide	Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay	[PMID: 35635954]
NAMALVA	IC₅₀	0.03 μM Compound: 2	Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 23168019]
NCI-H929	CC₅₀	0.035 μM Compound: Pomalidomide	Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay	[PMID: 30684871]
PBMC	IC₅₀	0.013 μM Compound: 2	Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA	[PMID: 23168019]
T-cell	EC₅₀	0.008 μM Compound: 2	Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA	[PMID: 23168019]

In Vitro

Pomalidomide also inhibits Whole Blood TNF-α with IC₅₀ of 25 nM^[1]. Exposure of lymphoma cells to Pomalidomide (CC-4047) leads to 40% decrease in cell proliferation when compared with vehicle-treated controls. Pomalidomide inhibits by 40% the DNA synthesis of Raji cells (P=0.036)^[2]. In both CD4⁺ and CD8⁺ cells, Pomalidomide (CC-4047) is the most potent IL-2-elevator, followed by CC-6032 and CC-5013. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10, and slightly more potent than CC-5013 at elevating IFN-γ^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The administration of Pomalidomide (CC-4047) for two consecutive days before mAb therapy enhances the antitumor activity of Rituximab and doubled the median survival of lymphoma-bearing mice. Statistically, significant differences are observed between animals treated with Rituximab versus Pomalidomide+Rituximab. The median survival time of animals treated with Pomalidomide and Rituximab is longer (median survival, 74 days; 95% CI, 70-78) than those treated with Rituximab monotherapy (median survival, 38 days; 95% CI, 26-50; log-rank test, P=0.002). The administration of CC-5013 or Pomalidomide for two consecutive days leads to a significant increase in the number of circulating NK cells as shown by flow cytometry analysis, in lymphoma-bearing SCID mice^[2]. Following a 50 mg/kg PO administration of Pomalidomide (POM) to rats, unbound concentrations in blood reach a C_max value of 1100±82 ng/mL at 4.6±2.4 hours, with a concomitant AUC_(0-10) value of 6800±2000 ng hr/mL. Unbound POM in the brain, however, has a C_max value of 430±63 ng/mL at 4.1±1.5 hours and an AUC_(0-10) value of 2700±740 ng hr/mL, giving an unbound AUC_brain to AUC_blood ratio of 0.39±0.03. These values are consistent with excellent blood-brain-barrier penetration. The results obtained in this study are consistent with those seen in a concurrent study looking at whole brain POM content following its oral administration to mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

273.24

Formula

C₁₃H₁₁N₃O₄

CAS No.

19171-19-8

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1N(C(C2=C1C=CC=C2N)=O)C(C(N3)=O)CCC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (182.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6598 mL	18.2989 mL	36.5979 mL
5 mM	0.7320 mL	3.6598 mL	7.3196 mL
10 mM	0.3660 mL	1.8299 mL	3.6598 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (36.60 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (285 KB) SDS (418 KB)

COA (252 KB) HNMR (119 KB) RP-HPLC (144 KB)

Handling Instructions (2659 KB)

References

[1]. Zhu YX, et al. Molecular mechanism of action of the immune-modulatory drugs, thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7. [Content Brief]

[2]. Hernandez-Ilizaliturri FJ1, et al. Immunomodulatory drug CC-5013 or CC-4047 and rituximab enhance antitumor activity in a severe combined immunodeficient mouse lymphoma model. Clin Cancer Res. 2005 Aug 15;11(16):5984-92. [Content Brief]

[3]. Schafer PH, et al. Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs. J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32. [Content Brief]

[4]. Li Z, et al. Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models. PLoS One. 2013 Aug 5;8(8):e71754. [Content Brief]

[5]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief]

[6]. Liu D, et al. Tumour necrosis factor-α inhibits hepatic lipid deposition through GSK-3β/β-catenin signaling in juvenile turbot (Scophthalmus maximus L.). Gen Comp Endocrinol. 2016 Mar 1;228:1-8. [Content Brief]

Cell Assay ^[2]	Lymphoma cell lines are placed in 96-well plates (1×10⁵ cells per well) and exposed to escalating concentrations of CC-5013, Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL), or vehicle control single agents or in combination with Rituximab or Trastuzumab (isotype), at a final antibody concentration of 10 μg/mL. The final concentration is adjusted to 200 μL with 10% RPMI. The cell lines are incubated at 37°C and 5% CO₂ for 24 and 48 hours. Following 24 or 48 hours, 1 μCi per well of [³H]-thymidine is added and cells are incubated for 18 hours more. Cells are then harvested using the Harvest system into the 96-well glass filters and [³H]-thymidine uptake is measured using an automated scintillation counter. Each experiment is done in triplicate at three different times; results are presented as the mean of counts per minute (cpm) at 24 and 48 hours±SD^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[4]	Mice^[2] Six- to 8-week-old SCID mice are used for this purpose. On day 0, all the animals receive 1×10⁶ Raji cells via tail vein injection. After 72 hours of tumor engraftment, the animals are divided into seven cohorts. The first cohort (group A) serve as control and receive no treatment. Groups B and C consist of animals treated with either CC-5013 (0.5 mg/kg) or Pomalidomide (0.5 mg/kg) given i.p. on days +3, +4, +8, +9, +13, +14, +18, and +19. Groups D and E are treated with Rituximab or Trastuzumab (isotype control) monotherapy given via tail vein injection at 10 mg/kg on days +5, +10, +15, and +20. Finally, groups F and G consist of animals treated with Rituximab in combination with CC-5013 (group E) or Pomalidomide (group G). IMiDs are given i.p. for two consecutive days before each dose of Rituximab. After completion of therapy, animals are observed for a period of 90 days. The end point of the study is survival defined as the time for the development of limb paralysis. Animals that reach the end point or survived after 3 months of observation are sacrificed by cervical dislocation. Pathologic examination of all organs (liver, lung, and brain) is done to detect any residual disease. The experiments are repeated in three separate occasions. Rats^[4] A total of 3 male CD-IGS rats are used. Pomalidomide is administered as a single PO administration via the stomach cannula, at 50 mg/kg (5 mL/kg) in a 0.5% carboxymethylcellulose/0.25% Tween 80 suspension formulation. Microdialysate is collected in a cooling fraction collector, set at 4°C at intervals of 25 minutes for 10 hours after dosing. To calculate AUC, the corrected concentration of each sample is multiplied by the interval over which the sample is collected; in this case 25 minutes, and divided by 60 minutes per hour. The sum of these values represented the total AUC value over the specified time range. To generate graphs, the concentration at each time point is plotted at the mid-point of each collection interval. Microdialysates are collected at the specified time points and analyzed for Pomalidomide concentration using a LC-MS/MS assay, within 12 hours. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhu YX, et al. Molecular mechanism of action of the immune-modulatory drugs, thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7. [Content Brief] [2]. Hernandez-Ilizaliturri FJ1, et al. Immunomodulatory drug CC-5013 or CC-4047 and rituximab enhance antitumor activity in a severe combined immunodeficient mouse lymphoma model. Clin Cancer Res. 2005 Aug 15;11(16):5984-92. [Content Brief] [3]. Schafer PH, et al. Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs. J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32. [Content Brief] [4]. Li Z, et al. Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models. PLoS One. 2013 Aug 5;8(8):e71754. [Content Brief] [5]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief] [6]. Liu D, et al. Tumour necrosis factor-α inhibits hepatic lipid deposition through GSK-3β/β-catenin signaling in juvenile turbot (Scophthalmus maximus L.). Gen Comp Endocrinol. 2016 Mar 1;228:1-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6598 mL	18.2989 mL	36.5979 mL	91.4947 mL
	5 mM	0.7320 mL	3.6598 mL	7.3196 mL	18.2989 mL
	10 mM	0.3660 mL	1.8299 mL	3.6598 mL	9.1495 mL
	15 mM	0.2440 mL	1.2199 mL	2.4399 mL	6.0996 mL
	20 mM	0.1830 mL	0.9149 mL	1.8299 mL	4.5747 mL
	25 mM	0.1464 mL	0.7320 mL	1.4639 mL	3.6598 mL
	30 mM	0.1220 mL	0.6100 mL	1.2199 mL	3.0498 mL
	40 mM	0.0915 mL	0.4575 mL	0.9149 mL	2.2874 mL
	50 mM	0.0732 mL	0.3660 mL	0.7320 mL	1.8299 mL
	60 mM	0.0610 mL	0.3050 mL	0.6100 mL	1.5249 mL
	80 mM	0.0457 mL	0.2287 mL	0.4575 mL	1.1437 mL
	100 mM	0.0366 mL	0.1830 mL	0.3660 mL	0.9149 mL

Pomalidomide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pomalidomide19171-19-8CC-4047CC4047CC 4047Ligands for E3 LigaseMolecular GluesApoptosisE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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Pomalidomide (Synonyms: CC-4047)

Customer Review

Other Forms of Pomalidomide:

Pomalidomide Related Antibodies

16 Publications Citing Use of MCE Pomalidomide

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Ligands for E3 Ligase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Pomalidomide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pomalidomide Related Classifications

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