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Description: Sardomozide (formerly SAM-486A; CGP-48664) is a novel and 2nd-generation polyamine synthesis inhibitor and S-adenosylmethionine decarboxylase (SAMDC) inhibitor with a broad spectrum antiproliferative and antitumor activity. 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.
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| ln Vitro |
An IC50 of 5 nM was observed in a cell experiment for the S-adenosylmethionine decarboxylase (SAMDC) inhibitor sardomozide. After being treated with 3 μM Sardomozide for 48 hours, intracellular SAMDC activity drops to 10% of the control level[1]. Vacuole production is not seen in CHO/664 cells grown in the presence of Sardomozide and treated with DENSPM; instead, the cells exhibit growth inhibition and DENSPM levels comparable to those of the original CHO cells[2].
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| Additional Infomation |
Sardomozide is a methylglyoxal bis(guanidinohydrazone) (MGBG) derivative with potential antitumor and antiviral activities. Sardomozide selectively binds to and inhibits S-adenosylmethionine decarboxylase (SAMDC), an enzyme essential for the synthesis of polyamines such as spermine and spermidine, which bind to DNA and play crucial roles in cell division, cell differentiation, and membrane function. By inhibiting SAMDC, sardomozide reduces intracellular polyamine concentrations, thereby interfering with cell growth and differentiation. Furthermore, the drug also exerts its anti-HIV effect by inhibiting the expression of eukaryotic translation initiation factor 5A (eIF-5A), which is essential for retroviral replication.
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| Molecular Formula |
C11H14N6
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| Molecular Weight |
230.28
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| Exact Mass |
230.128
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| CAS # |
149400-88-4
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| Related CAS # |
Sardomozide dihydrochloride;138794-73-7
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| PubChem CID |
9576789
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| Appearance |
Off-white to light yellow solid
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| Density |
1.54g/cm3
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| Boiling Point |
490.6ºC at 760mmHg
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| Flash Point |
250.5ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.768
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| LogP |
2.095
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N=C(C1=CC=CC2=C1CC/C2=N\NC(N)=N)N
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| InChi Key |
CYPGNVSXMAUSJY-CXUHLZMHSA-N
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| InChi Code |
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+
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| Chemical Name |
Hydrazinecarboximidamide, 2-(4-(aminoiminomethyl)-2,3-dihydro-1H-inden-1-ylidene)-
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| Synonyms |
CGP 48664 SAM-486ACGP-48664 SAM486A CGP48664 SAM 486ASAM486A SAM-486A SAM 486A
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~16.7 mg/mL (~72.4 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (7.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (16.7 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (7.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (16.7 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3425 mL | 21.7127 mL | 43.4254 mL | |
| 5 mM | 0.8685 mL | 4.3425 mL | 8.6851 mL | |
| 10 mM | 0.4343 mL | 2.1713 mL | 4.3425 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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