SML3185

CGP 48664 dihydrochloride

≥98% (HPLC)

• Synonym(s): (E)-2-(4-carbamimidoyl-2,3-dihydro-1H-inden-1-ylidene)hydrazine-1-carboximidamide dihydrochloride, (E)-2-[4-(Aminoiminomethyl)-2,3-dihydro-1H-inden-1-ylidene]hydrazinecarboximidamide dihydrochloride, 4-Amidino-1-indanone-2′-amidinohydrazone dihydrochloride, 4-Amidinoindan-1-one-2?-amidinohydrazone dihydrochloride, CGP 48664A dihydrochloride, CGP48664 dihydrochloride, CMA 48664 dihydrochloride, SAM486A dihydrochloride, Sardomozide dihydrochlorid, Sardomozide dihydrochloride
• Empirical Formula (Hill Notation): C₁₁H₁₄N₆ · 2HCl
• CAS Number: 138794-73-7
• Molecular Weight: 303.19
• MDL number: MFCD00910325
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: −20°C
• SMILES string: NC(C1=CC=CC2=C1CC/C2=N\NC(N)=N)=N.Cl.Cl
• InChI: 1S/C11H14N6/c12-10(13)8-3-1-2-7-6(8)4-5-9(7)16-17-11(14)15/h1-3H,4-5H2,(H3,12,13)(H4,14,15,17)/b16-9+
• InChI key: CYPGNVSXMAUSJY-CXUHLZMHSA-N

Description

Biochem/physiol Actions

CGP 48664 (SAM486A; Sardomozide) is a polyamine (PA) biosynthesis inhibitor (73% and 97% downregulation of murine leukemia L1210 cellular spermidine and spermine, respectively, by 0.5 μM Sardomozide in 4 days) that targets the rate-limiting enzyme S-adenosylmethionine decarboxylase (AdoMetDC, SAMDC, AMD1) in a potent (IC50 = 5 nM against rat AMD1) and selective manner with little or no inhibitory efficacy toward diamine oxidase or ornithine decarboxylase (IC50 = 18 μM and >50 μM against rat DAO and ODC, respectively). CGP 48664 effectively inhibits the proliferation of murine (GI50 = 0.5 μM against L1210 in 4 days) and human cancer cell lines in cultures (GI50 from 0.26 to 0.6 μM in 5 days; GI50 = 0.8 μM against human melanoma SK MEL-24 in 10 days) and suppresses the growth of murine and human tumor xenografts in mice in vivo (ED50 ≤0.5 mg/kg i.p.). CGP 48664 (Sardomozide) potently inhibits growth of PFA ependymoma cells.

Potent and selective S-adenosylmethionine decarboxylase (AdoMetDC, SAMDC, AMD1) inhibitor with anti-cancer efficacy both in vitro and in vivo.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable