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Sardomozide dihydrochloride

Names

[ CAS No. ]:
138794-73-7

[ Name ]:
Sardomozide dihydrochloride

[Synonym ]:
Sardomozide
(1E)-1-[(Diaminomethylene)hydrazono]-4-indanecarboximidamide
1H-Indene-4-carboximidamide, 1-[2-(diaminomethylene)hydrazinylidene]-2,3-dihydro-, (1E)-
Sardomozide dihydrochloride

Biological Activity

[Description]:

Sardomozide dihydrochloride is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Cancer

[Target]

IC50: 5 nM (SAMDC)[1]


[In Vitro]

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[1]. 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[2].

[Cell Assay]

The parent CHO cell line is chronically exposed to increasing levels of Sardomozide for at least eight passages beginning at 0.1 μM. Cell lines are serially exposed to increasing concentrations until a panel of sublines is obtained resistant to 1 (CHO/1). 3 (CHO/3), 10 (CHO/10), 30 (CHO/30), and 100 (CHO/100) μM Sardomozide for comparative studies[2].

[References]

[1]. Regenass U, et al. CGP 48664, a new S-adenosylmethionine decarboxylase inhibitor with broad spectrum antiproliferative and antitumor activity. Cancer Res. 1994 Jun 15;54(12):3210-7.

[2]. Kramer DL, et al. Lysosomal sequestration of polyamine analogues in Chinese hamster ovary cells resistant to the S-adenosylmethionine decarboxylase inhibitor, CGP-48664. Cancer Res. 1998 Sep 1;58(17):3883-90.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
490.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C11H16Cl2N6

[ Molecular Weight ]:
303.19

[ Flash Point ]:
250.5±31.5 °C

[ LogP ]:
-0.49

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.768

[ Storage condition ]:
2-8℃


Related Compounds