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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(guanylhydrazone) (MGBG) derivative with potential antineoplastic and antiviral properties. Sardomozide selectively binds to and inhibits S-adenosylmethionine decarboxylase (SAMDC), an enzyme essential for the biosynthesis of polyamines, such as spermine and spermidine that bind to DNA and play critical roles in cell division, cell differentiation and membrane function. By inhibiting SAMDC, sardomozide reduces the intracellular polyamine concentration, thereby interfering with cell growth and differentiation. In addition, this agent also exhibits anti-HIV effect via suppressing 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 |
Typically exists as solid at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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