WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H201614
CAS#: 881202-45-5
Description: Serdemetan, also known as JNJ-26854165, is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. HDM2 antagonist JNJ-26854165 inhibits the binding of the HDM2–p53 complex to the proteasome, blocking the degradation of p53; p53 signaling and p53-mediated induction of tumor cell apoptosis may thus be restored. In addition to p53, degradation of other HDM2 client proteins may be inhibited.
Hodoodo Cat#: H201614
Name: Serdemetan
CAS#: 881202-45-5
Chemical Formula: C21H20N4
Exact Mass: 328.17
Molecular Weight: 328.410
Elemental Analysis: C, 76.80; H, 6.14; N, 17.06
Synonym: JNJ26854165; JNJ-26854165; JNJ 26854165; Serdemetan.
IUPAC/Chemical Name: N1-(2-(1H-indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diamine
InChi Key: CEGSUKYESLWKJP-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: C1(NCCC2=CNC3=C2C=CC=C3)=CC=C(NC4=CC=NC=C4)C=C1
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 328.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Lehman JA, Hauck PM, Gendron JM, Batuello CN, Eitel JA, Albig A, Kadakia MP, Mayo LD. Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. PLoS One. 2013 Sep 6;8(9):e74741. doi: 10.1371/journal.pone.0074741. eCollection 2013. PubMed PMID: 24040331; PubMed Central PMCID: PMC3765416.
2: Jones RJ, Gu D, Bjorklund CC, Kuiatse I, Remaley AT, Bashir T, Vreys V, Orlowski RZ. 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. doi: 10.1124/jpet.113.204958. Epub 2013 Jul 2. Erratum in: J Pharmacol Exp Ther. 2013 Nov;347(2):540. PubMed PMID: 23820125; PubMed Central PMCID: PMC3876782.
3: Chargari C, Leteur C, Angevin E, Bashir T, Schoentjes B, Arts J, Janicot M, Bourhis J, Deutsch E. 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. doi: 10.1016/j.canlet.2011.08.011. Epub 2011 Aug 22. PubMed PMID: 21937165.
4: Smith MA, Gorlick R, Kolb EA, Lock R, Carol H, Maris JM, Keir ST, Morton CL, Reynolds CP, Kang MH, Arts J, Bashir T, Janicot M, Kurmasheva RT, Houghton PJ. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Aug;59(2):329-32. doi: 10.1002/pbc.23319. Epub 2011 Sep 15. PubMed PMID: 21922647.
5: Tabernero J, Dirix L, Schöffski P, Cervantes A, Lopez-Martin JA, Capdevila J, van Beijsterveldt L, Platero S, Hall B, Yuan Z, Knoblauch R, Zhuang SH. A phase I first-in-human pharmacokinetic and pharmacodynamic study of serdemetan in patients with advanced solid tumors. Clin Cancer Res. 2011 Oct 1;17(19):6313-21. doi: 10.1158/1078-0432.CCR-11-1101. Epub 2011 Aug 10. PubMed PMID: 21831953.
6: Yuan Y, Liao YM, Hsueh CT, Mirshahidi HR. Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP. J Hematol Oncol. 2011 Apr 20;4:16. doi: 10.1186/1756-8722-4-16. Review. PubMed PMID: 21504625; PubMed Central PMCID: PMC3103487.
7: Millard M, Pathania D, Grande F, Xu S, Neamati N. Small-molecule inhibitors of p53-MDM2 interaction: the 2006-2010 update. Curr Pharm Des. 2011;17(6):536-59. Review. PubMed PMID: 21391905.
8: Kojima K, Burks JK, Arts J, Andreeff M. The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Mol Cancer Ther. 2010 Sep;9(9):2545-57. doi: 10.1158/1535-7163.MCT-10-0337. Epub 2010 Aug 24. PubMed PMID: 20736344; PubMed Central PMCID: PMC2949269.
9: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Apr;31(3):183-226. PubMed PMID: 19536362.
