1. PROTAC
    Apoptosis
  2. Ligand for E3 Ligase
    Apoptosis
  3. Pomalidomide

Pomalidomide (Synonyms: CC-4047)

Cat. No.: HY-10984 Purity: 99.96%
Handling Instructions

Pomalidomide is the third-generation immunomodulatory agent, functions through interacting 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

Pomalidomide Chemical Structure

CAS No. : 19171-19-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
Estimated Time of Arrival: December 31
100 mg USD 108 In-stock
Estimated Time of Arrival: December 31
200 mg USD 120 In-stock
Estimated Time of Arrival: December 31
500 mg USD 140 In-stock
Estimated Time of Arrival: December 31
1 g USD 180 In-stock
Estimated Time of Arrival: December 31
5 g USD 450 In-stock
Estimated Time of Arrival: December 31
10 g   Get quote  
50 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Pomalidomide purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.

    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 MCE. Usage Cited in: Gen Comp Endocrinol. 2015 Dec 30;228:1-8.

    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).

    View All Ligand for E3 Ligase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

    IC50 & Target[5]

    Cereblon

     

    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].

    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 Cmax 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 Cmax 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 AUCbrain to AUCblood 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].

    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

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (365.98 mM)

    *"≥" means soluble, but saturation unknown.

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    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

    Purity: 99.96%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    PomalidomideCC-4047CC4047CC 4047Ligand for E3 LigaseApoptosisE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Pomalidomide
    Cat. No.:
    HY-10984
    Quantity:
    MCE Japan Authorized Agent: