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JNJ-26854165 (Serdemetan)

P53 activator, blocking Mdm2-p53 interaction CAS# 881202-45-5

JNJ-26854165 (Serdemetan)

Catalog No. BCC2240----Order now to get a substantial discount!

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JNJ-26854165 (Serdemetan): 5mg $92 In Stock
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Chemical structure

JNJ-26854165 (Serdemetan)

3D structure

Chemical Properties of JNJ-26854165 (Serdemetan)

Cas No. 881202-45-5 SDF Download SDF
PubChem ID 11609586 Appearance Powder
Formula C21H20N4 M.Wt 328.41
Type of Compound N/A Storage Desiccate at -20°C
Synonyms JNJ-26854165
Solubility DMSO : 50 mg/mL (152.25 mM; Need ultrasonic)
Chemical Name 1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine
SMILES C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
Standard InChIKey CEGSUKYESLWKJP-UHFFFAOYSA-N
Standard InChI InChI=1S/C21H20N4/c1-2-4-21-20(3-1)16(15-24-21)9-14-23-17-5-7-18(8-6-17)25-19-10-12-22-13-11-19/h1-8,10-13,15,23-24H,9,14H2,(H,22,25)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of JNJ-26854165 (Serdemetan)

DescriptionJNJ-26854165 (Serdemetan) is an antagonist of HDM2 ubiquitin ligase and also inducer of early apoptosis in p53 wild-type cells,
TargetsHDM2Mdm2    

JNJ-26854165 (Serdemetan) Dilution Calculator

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JNJ-26854165 (Serdemetan) Molarity Calculator

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Preparing Stock Solutions of JNJ-26854165 (Serdemetan)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.045 mL 15.2249 mL 30.4497 mL 60.8995 mL 76.1244 mL
5 mM 0.609 mL 3.045 mL 6.0899 mL 12.1799 mL 15.2249 mL
10 mM 0.3045 mL 1.5225 mL 3.045 mL 6.0899 mL 7.6124 mL
50 mM 0.0609 mL 0.3045 mL 0.609 mL 1.218 mL 1.5225 mL
100 mM 0.0304 mL 0.1522 mL 0.3045 mL 0.609 mL 0.7612 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on JNJ-26854165 (Serdemetan)

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

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

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.

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References on JNJ-26854165 (Serdemetan)

Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.[Pubmed:21922647]

Pediatr Blood Cancer. 2012 Aug;59(2):329-32.

JNJ-26854165 was originally developed as an activator of p53 capable of inducing apoptosis in cancer cell lines. In vitro, JNJ-26854165 demonstrated cytotoxic activity. The ALL cell line panel had a significantly lower median IC(50) (0.85 microM) than the remaining cell lines. In vivo JNJ-26854165 induced significant differences in EFS distribution compared to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable ALL xenografts. Objective responses were observed in 4 of 37 solid tumor xenografts, and 2 of 7 ALL xenografts achieved PR or CR. Responses were noted in xenografts with both mutant and wild-type p53.

Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.[Pubmed:21937165]

Cancer Lett. 2011 Dec 22;312(2):209-18.

Serdemetan (JNJ-26854165) is a novel tryptamine compound with antiproliferative activity in various p53 wild-type (WT) tumor cell lines. We investigated its potential as radiosensitizer using four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. Serdemetan inhibited clonogenic survival in all cell lines, but in a lower extent in p53-null-HCT116. In the combination studies, Serdemetan treatment at 0.25muM in H460 and at 5muM in A549 cells resulted in a sensitivity-enhancement ratio of 1.18 and 1.36, respectively. At 2Gy, surviving fractions were 0.72 and 0.97 for p53-WT HCT116 and p53-null cells exposed to 0.5muM of Serdemetan, respectively (p<0.05). Radiosensitization of H460 and A549 cells was associated with G2/M cell cycle arrest and with an increased expression of p53 and p21. In vivo, Serdemetan caused a greater than additive increase in tumor growth delay. The dose enhancement factor was 1.9 and 1.6 for H460 and A549 tumors, respectively. Serdemetan inhibited proliferation, capillary tube formation and migration of HMEC-1 cells. These effects were more marked concurrently with irradiation. These results in tumor and endothelial cells suggest that Serdemetan has potential as a radiosensitizer. Further investigations are warranted with regard to the molecular mechanisms underlying its actions and its dependency regarding p53 status.

Description

Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

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