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Sardomozide dihydrochloride

Cat. No. M9475
Sardomozide dihydrochloride Structure
Synonym:

Sardomozide 2HCl; CGP 48664A

Size Price Availability
5mg USD 135  USD135 Custom Synthesis
10mg USD 235  USD235 Custom Synthesis
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Quality Control & Documentation
Biological Activity

Sardomozide dihydrochloride (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). Sardomozide inhibits SAMDC with an IC50 of 5 nM in cell assay. Intracellular SAMDC activity is reduced to 10% of control after treatment for 48 hours with 3 μM Sardomozide.

Chemical Information
Molecular Weight 303.19
Formula C11H16Cl2N6
CAS Number 138794-73-7
Solubility (25°C) DMSO ≥ 10 mg/mL
Water ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Koomoa DL, et al. Mol Cancer Ther. Inhibition of S-adenosylmethionine decarboxylase by inhibitor SAM486A connects polyamine metabolism with p53-Mdm2-Akt/protein kinase B regulation and apoptosis in neuroblastoma.

[2] Millward MJ, et al. Invest New D rugs. Multi-centre Phase II trial of the polyamine synthesis inhibitor SAM486A (CGP48664) in patients with metastatic melanoma.

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Keywords: Sardomozide dihydrochloride, Sardomozide 2HCl; CGP 48664A supplier, inhibitors, activators


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