Art. -Nr.: HY-12025

Serdemetan

(Synonyms: JNJ-26854165)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 99.56%
CAS. Nr.: 881202-45-5
Formel: C₂₁H₂₀N₄
Molecular Weight:328.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Serdemetan Chemical Structure

CAS. Nr.: 881202-45-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 881202-45-5
Appearance Solid
Molecular Weight 328.41
Formel C₂₁H₂₀N₄
Color Light brown to brown
SMILES

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

JNJ-26854165
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

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Journal Impact Factor

Biochem Pharmacol

PLCE1 enhances mitochondrial dysfunction to promote GSDME-mediated pyroptosis in doxorubicin-induced cardiotoxicity. [Abstract]

2024 May:223:116142. PMID: 38499110
Cells

PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]

2026 Mar 5;15(5):473. PMID: 41827906
Toxicol Appl Pharmacol

In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]

2024 May:486:116945. PMID: 38688424

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0450 mL

15.2249 mL

30.4497 mL

5 mM

0.6090 mL

3.0450 mL

6.0899 mL

10 mM

0.3045 mL

1.5225 mL

3.0450 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.61 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chargari C, et, al. Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts. Cancer Lett. 2011 Dec 22;312(2):209-18. [Content Brief]

[2]. Lehman JA, et, al. Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. PLoS One. 2013 Sep 6;8(9):e74741. [Content Brief]

[3]. Jones RJ, et, al. The novel anticancer agent JNJ-26854165 induces cell death through inhibition of cholesterol transport and degradation of ABCA1. J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Serdemetan

3 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Serdemetan

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Serdemetan Related Classifications

HY-12025 Related Classifications