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JNJ-26854165 (Serdemetan) (Synonyms: Serdemetan)

Catalog No.GC12117

An antagonist of MDM2 action

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JNJ-26854165 (Serdemetan) Chemical Structure

Cas No.: 881202-45-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$69.00
In stock
5mg
$57.00
In stock
25mg
$195.00
In stock
100mg
$477.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

H460, A549 cells, and HMEC-1 endothelial cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5, 1, 2.5, 5, 10, 25 and 50 μM; 48 h

Applications

After 48 h treatment, Serdemetan inhibited cell proliferation with IC50 values of 3.9 μM, and 8.7 μM for H460 cells and A549 cells, respectively. Moreover, Serdemetan at 5 μM inhibited HMEC-1 endothelial cell migration.

Animal experiment [1]:

Animal models

H460 and A549 cells, injected in the right flank of nude mice were grown as tumor xenografts.

Dosage form

50 mg/kg; p.o. twice a week, for 2 weeks

Applications

Serdemetan treatment significantly enhanced radiation-induced growth delays in A549 and H460 xenograft tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Chargari, C., Leteur, C., Angevin, E., Bashir, T., Schoentjes, B., Arts, J., Janicot, M., Bourhis, J. and Deutsch, E. (2011) Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts. Cancer Lett. 312, 209-218

Background

JNJ-26854165, also named as Serdemetan, is originally developed as an activator of p53, is now regarded as a novel oral Human Double Minute-2 (HDM-2) ubiquitin ligase antagonist. It can increase the level of HDM-2 client proteins, such as p53, by inhibiting the association of HDM-2-client protein complex with the proteosome. It is demonstrated potent anti-proliferative and apoptosis-inducing activity of JNJ-26854165 in a broad range of p53 wild type and mutant tumor models. In vivo, JNJ-26854165 may induce important differences in EFS distribution when comparing to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable ALL xenografts.

Reference

[1].J. Tabernero, L. Dirix, P. Schoffski, A. Cervantes, J. Capdevila, J. Baselga, L. van Beijsterveldt, H. Winkler, S. Kraljevic and S. H. Zhuang. Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of HDM-2 antagonist JNJ-26854165 in patients with advanced refractory solid tumors. Journal of Clinical Oncology (Meeting Abstracts) May 2009 vol. 27 no. 15S 3514
[2].Malcolm A. Smith, Richard Gorlick, E. Anders Kolb, Richard Lock, Hernan Carol, John M. Maris, Stephen T. Keir, Christopher L. Morton, C. Patrick Reynolds, Min H. Kang, Janine Arts, Tarig Bashir, Michel Janicot, Raushan T. Kurmasheva, Peter J. Houghton. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. Pediatric Blood & Cancer. Volume 59, Issue 2, pages 329–332, August 2012.

Chemical Properties

Cas No. 881202-45-5 SDF
Synonyms Serdemetan
Chemical Name 1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine
Canonical SMILES C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
Formula C21H20N4 M.Wt 328.41
Solubility ≥ 14.8 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.045 mL 15.2249 mL 30.4497 mL
5 mM 0.609 mL 3.045 mL 6.0899 mL
10 mM 0.3045 mL 1.5225 mL 3.045 mL
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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