Sardomozide HCl, also known as SAM486A or CGP48664, is a second-generation polyamine synthesis inhibitor, which inhibits the activity of the polyamine biosynthetic enzyme S-adenosylmethionine decarboxylase (SAMDC). SAM486 is more potent and specific than the first-generation SAMDC inhibitor methylglyoxal (bis) guanylhydrazone (MGBG). Preclinical testing confirmed promising antiproliferative activity. The in vitro tests showed that p53 wild-type NB cells were highly sensitive to SAM486A treatment. Most notably, SAM486A treatment resulted in the rapid accumulation of proapoptotic proteins p53 and Mdm2.
CAS Number: 138794-73-7
Molecular Weight: 303.19
Chemical Name: (E)-2-(4-carbamimidoyl-2,3-dihydro-1H-inden-1-ylidene)hydrazinecarboximidamide dihydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Sardomozide is a S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM in cell assay. Following treatment for 48 h with 3 μM Sardomozide, intracellular SAMDC activity is reduced to 10% of control. When the CHO/664 cells are grown in the presence of Sardomozide and during treatment with DENSPM, vacuole formation is not observed, and these cells are growth-inhibited and contain levels of DENSPM similar to the parental CHO cells.
- Millward MJ, Joshua A, Kefford R, Aamdal S, Thomson D, Hersey P, Toner G, Lynch K. Multi-centre Phase II trial of the polyamine synthesis inhibitor SAM486A (CGP48664) in patients with metastatic melanoma. Invest New Drugs. 2005 Jun;23(3):253-6. PubMed PMID: 15868382.
- Hu X, Washington S, Verderame MF, Demers LM, Mauger D, Manni A. Biological activity of the S-adenosylmethionine decarboxylase inhibitor SAM486A in human breast cancer cells in vitro and in vivo. Int J Oncol. 2004 Dec;25(6):1831-8. PubMed PMID: 15547724.
- Koomoa DL, Borsics T, Feith DJ, Coleman CC, Wallick CJ, Gamper I, Pegg AE, Bachmann AS. Inhibition of S-adenosylmethionine decarboxylase by inhibitor SAM486A connects polyamine metabolism with p53-Mdm2-Akt/protein kinase B regulation and apoptosis in neuroblastoma. Mol Cancer Ther. 2009 Jul;8(7):2067-75. doi: 10.1158/1535-7163.MCT-08-1217. Epub 2009 Jul 7. PubMed PMID: 19584241; PubMed Central PMCID: PMC2731875.
Products are for research use only. Not for human use.
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