Cas：138794-73-7 (HCl salt)
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.
Chemical Formula: C11H16Cl2N6
Molecular Weight: 303.19
Elemental Analysis: C, 43.58; H, 5.32; Cl, 23.38; N, 27.72
Appearance: White to off 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 water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in water
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
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.
- 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.
- 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.
- van Zuylen L, Bridgewater J, Sparreboom A, Eskens FA, de Bruijn P, Sklenar I, Planting AS, Choi L, Bootle D, Mueller C, Ledermann JA, Verweij J. Phase I and pharmacokinetic study of the polyamine synthesis inhibitor SAM486A in combination with 5-fluorouracil/leucovorin in metastatic colorectal cancer. Clin Cancer Res. 2004 Mar 15;10(6):1949-55. PubMed PMID: 15041711.
- Pless M, Belhadj K, Menssen HD, Kern W, Coiffier B, Wolf J, Herrmann R, Thiel E, Bootle D, Sklenar I, MÃ¼ller C, Choi L, Porter C, Capdeville R. Clinical efficacy, tolerability, and safety of SAM486A, a novel polyamine biosynthesis inhibitor, in patients with relapsed or refractory non-Hodgkin's lymphoma: results from a phase II multicenter study. Clin Cancer Res. 2004 Feb 15;10(4):1299-305. PubMed PMID: 14977828.
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