1. Apoptosis Metabolic Enzyme/Protease
  2. MDM-2/p53 E1/E2/E3 Enzyme Apoptosis
  3. Serdemetan

Serdemetan  (Synonyms: JNJ-26854165)

Cat. No.: HY-12025 Purity: 99.81%
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Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes.

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

Serdemetan Chemical Structure

Serdemetan Chemical Structure

CAS No. : 881202-45-5

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10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 88 In-stock
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10 mg USD 130 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes[1][2][3].

In Vitro

Serdemetan (0.5-50 μM; 48-72 h) inhibits cell proliferation of H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells in a dose-dependent manner[1].
Serdemetan (0.25-5 μM; 48 h) triggers cell arrests in G2/M phase of A549 cells and H460 cells[1].
Serdemetan (0.5-10 μM; 48 h) increases expression of p53 and p21 in H460, A549 and p53-WT HCT116 cells[1].
Serdemetan (0.25-10 μM; 12-14 d) affects clonogenic survival in H460, A549 p53-WT HCT116 and p53-null HCT116 cells[1].
Serdemetan (0.25-5 μM; 12-14 d) increases radiation-induced clonogenic inhibition[1].
Serdemetan (5-20 μM; 4-24 h) inhibits neovessels formation and delays scratch wound repair of HMEC-1 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells
Concentration: 0.5-50 μM
Incubation Time: 48, 72 hours
Result: Inhibited cell proliferation with IC50s of 3.9, 8.7, 0.97, 7.74, and 7.01 μM for H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells, respectively.

Western Blot Analysis[1]

Cell Line: H460, A549, HMEC-1, p53-WT HCT116, and p53-null HCT116 cells[1]
Concentration: 0.5 μM for A549 and p53-WT HCT11 cells; 5 μM for p53-null HCT116 and HMEC-1 cells; 10 μM for A549 cells
Incubation Time: Treated for 24 h exposure then cells were irradiated, western blots were performed on cells arrested 24 h after irradiation
Result: Slightly increased the expression of p53 and p21 in H460, A549, p53-WT HCT116.
Increased both p53 and p21 expression 24 h after the last drug exposure.
In Vivo

Serdemetan (50 mg/kg) enhances radiation-induced growth delays in H460 and A549 xenograft tumors[1].

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

Clinical Trial
Molecular Weight

328.41

Formula

C21H20N4

CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

C1(NCCC2=CNC3=C2C=CC=C3)=CC=C(C=C1)NC4=CC=NC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (152.25 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 3.0450 mL 15.2249 mL 30.4497 mL
5 mM 0.6090 mL 3.0450 mL 6.0899 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (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 (7.61 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.61 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(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 +
+
%
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0450 mL 15.2249 mL 30.4497 mL 76.1244 mL
5 mM 0.6090 mL 3.0450 mL 6.0899 mL 15.2249 mL
10 mM 0.3045 mL 1.5225 mL 3.0450 mL 7.6124 mL
15 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0750 mL
20 mM 0.1522 mL 0.7612 mL 1.5225 mL 3.8062 mL
25 mM 0.1218 mL 0.6090 mL 1.2180 mL 3.0450 mL
30 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5375 mL
40 mM 0.0761 mL 0.3806 mL 0.7612 mL 1.9031 mL
50 mM 0.0609 mL 0.3045 mL 0.6090 mL 1.5225 mL
60 mM 0.0507 mL 0.2537 mL 0.5075 mL 1.2687 mL
80 mM 0.0381 mL 0.1903 mL 0.3806 mL 0.9516 mL
100 mM 0.0304 mL 0.1522 mL 0.3045 mL 0.7612 mL
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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.

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Serdemetan
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