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MedKoo Cat#: 201614 | Name: Serdemetan
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Serdemetan, also known as JNJ-26854165, is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. Serdemetan inhibits the binding of the HDM2A–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.

Chemical Structure

Serdemetan
Serdemetan
CAS#881202-45-5

Theoretical Analysis

MedKoo Cat#: 201614

Name: Serdemetan

CAS#: 881202-45-5

Chemical Formula: C21H20N4

Exact Mass: 328.1688

Molecular Weight: 328.41

Elemental Analysis: C, 76.80; H, 6.14; N, 17.06

Price and Availability

Size Price Availability Quantity
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 3,750.00 2 Weeks
2g USD 4,850.00 2 Weeks
5g USD 6,750.00 2 Weeks
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Related CAS #
No Data
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, DMF, and ethanol
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
        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Serdemetan suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM). It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.
In vitro activity:
Serdemetan may function by inhibiting cholesterol transport, offering a potential treatment approach for mantle cell lymphoma (MCL) and multiple myeloma (MM). Serdemetan inhibited proliferation in both wild-type and mutant p53 cell lines, inducing S phase cell cycle arrest. Serdemetan treatment led to cholesterol accumulation in endosomes in certain cells. MM and MCL cells showed reduced cholesterol efflux and lysosomal storage disease characteristics. Reference: J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. https://pubmed.ncbi.nlm.nih.gov/23820125/
In vivo activity:
Serdemetan has potential as a radiosensitizer. 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. Reference: Cancer Lett. 2011 Dec 22;312(2):209-18. https://pubmed.ncbi.nlm.nih.gov/21937165/
Solvent mg/mL mM
Solubility
DMF 25.0 76.12
DMSO 20.0 60.90
Ethanol 1.0 3.04
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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:
1. 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. PMID: 23820125; PMCID: PMC3876782. 2. 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. PMID: 20736344; PMCID: PMC2949269. 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. PMID: 21937165. 4. 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. PMID: 21831953.
In vitro protocol:
1. 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. PMID: 23820125; PMCID: PMC3876782. 2. 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. PMID: 20736344; PMCID: PMC2949269.
In vivo protocol:
1. 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. PMID: 21937165. 2. 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. PMID: 21831953.
1: Park IA, Noh YK, Min KW, Kim DH, Lee JY, Son BK, Kwon MJ, Han MH, Hur JY, Pyo JS. p27 Cell Cycle Inhibitor and Survival in Luminal-Type Breast Cancer: Gene Ontology, Machine Learning, and Drug Screening Analysis. J Breast Cancer. 2024 Sep 4. doi: 10.4048/jbc.2024.0107. Epub ahead of print. PMID: 39344410. 2: Song Q, Wang P, Wu J, Lu M, Xia Q, Shi Y, Wang Z, Ma X, Zhao Q. Analysis of the role of CHPF in colorectal cancer tumorigenesis and immunotherapy based on bioinformatics and experiments. Discov Oncol. 2024 Sep 18;15(1):458. doi: 10.1007/s12672-024-01340-2. PMID: 39292317; PMCID: PMC11410747. 3: Kędzierski J, Jäger MC, Naeem S, Odermatt A, Smieško M. In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. Toxicol Appl Pharmacol. 2024 May;486:116945. doi: 10.1016/j.taap.2024.116945. Epub 2024 Apr 28. PMID: 38688424. 4: Wang X, Hong Y, Meng S, Gong W, Ren T, Zhang T, Liu X, Li L, Qiu L, Qian Z, Zhou S, Zhao M, Zhai Q, Meng B, Ren X, Zhang H, Wang X. A novel immune-related epigenetic signature based on the transcriptome for predicting the prognosis and therapeutic response of patients with diffuse large B-cell lymphoma. Clin Immunol. 2022 Oct;243:109105. doi: 10.1016/j.clim.2022.109105. Epub 2022 Aug 31. PMID: 36055572. 5: Huang W, Lin A, Luo P, Liu Y, Xu W, Zhu W, Wei T, Lyu Q, Guo L, Zhang J. EPHA5 mutation predicts the durable clinical benefit of immune checkpoint inhibitors in patients with lung adenocarcinoma. Cancer Gene Ther. 2021 Aug;28(7-8):864-874. doi: 10.1038/s41417-020-0207-6. Epub 2020 Aug 6. PMID: 32759987. 6: 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. PMID: 24040331; PMCID: PMC3765416. 7: 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. PMID: 23820125; PMCID: PMC3876782. 8: 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. PMID: 21937165. 9: 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. PMID: 21922647; PMCID: PMC4504194. 10: 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. PMID: 21831953.