1. PROTAC Apoptosis
  2. Ligands for E3 Ligase Molecular Glues Apoptosis
  3. Pomalidomide

Pomalidomide  (Synonyms: CC-4047)

Cat. No.: HY-10984 Purity: 99.85%
COA Handling Instructions

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

Pomalidomide Chemical Structure

CAS No. : 19171-19-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 66 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Pomalidomide:

Top Publications Citing Use of Products

    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).

    View All Ligands for E3 Ligase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    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].

    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 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].

    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.
    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
    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    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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    %
    Tween-80 +
    %
    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%

    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

    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.

    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
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    • 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.

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