Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C11H14N6 |
| Molecular Weight | 230.2691 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=N)N\N=C1/CCC2=C(C=CC=C12)C(N)=N
InChI
InChIKey=CYPGNVSXMAUSJY-CXUHLZMHSA-N
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+
Sardomozide (previously known as SAM486A or CGP-48664) was developed as an inhibitor of S-adenosyl-methionine-decarboxylase, a key enzyme for polyamine biosynthesis. Sardomozide possessed the broad-spectrum antiproliferative and antitumor activity. The drug participated in a phase II clinical trial as a monotherapy in patients with refractory or relapsed non-Hodgkin's lymphoma. In Phase II clinical trial in patients with metastatic melanoma, the drug didn’t have significant therapeutic potential. The further development of this drug was discontinued.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| 4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase. | 1993 Jul 23 |
|
| CGP 48664, a potent and specific S-adenosylmethionine decarboxylase inhibitor: effects on regulation and stability of the enzyme. | 1997 Feb 15 |
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| Inhibition of multidrug-resistant HIV-1 by interference with cellular S-adenosylmethionine decarboxylase activity. | 2006 Sep 15 |
|
| Inhibition of S-adenosylmethionine decarboxylase by inhibitor SAM486A connects polyamine metabolism with p53-Mdm2-Akt/protein kinase B regulation and apoptosis in neuroblastoma. | 2009 Jul |
Patents
Sample Use Guides
Forty-one previously treated patients with either diffuse large cell, follicular, or peripheral T-cell NHL were treated i.v. with 100 mg/m(2) SAM486A (SARDOMOZIDE) as a daily 1-h infusion for 5 days repeated every 3 weeks. Treatment was continued for a total of eight cycles or until disease progression.
Route of Administration:
Intravenous
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| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C2076
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NCI_THESAURUS |
C2090
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C1673
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1443105-76-7
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CHEMBL65789
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DTXSID40869976
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149400-88-4
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300000036894
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7678
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CEB05S0B9I
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9576789
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
