Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C17H19N5O2.C2H6O4S |
Molecular Weight | 451.497 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OCCS(O)(=O)=O.CCOC(=O)NC1=NC(N)=C2N=C([C@H](C)NC2=C1)C3=CC=CC=C3
InChI
InChIKey=JEFPWOBULVSOTM-PPHPATTJSA-N
InChI=1S/C17H19N5O2.C2H6O4S/c1-3-24-17(23)21-13-9-12-15(16(18)20-13)22-14(10(2)19-12)11-7-5-4-6-8-11;3-1-2-7(4,5)6/h4-10,19H,3H2,1-2H3,(H3,18,20,21,23);3H,1-2H2,(H,4,5,6)/t10-;/m0./s1
Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11561681
Mivobulin was given by 72 h continuous i.v. infusion at a dose of 4.5 mg/m2/day, days 1-3 every 21 days.
Route of Administration:
Intravenous
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NCI_THESAURUS |
C67421
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635370
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182762
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C1357
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8J08028R66
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HH-92
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C072383
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126268-81-3
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DTXSID50155130
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CHEMBL1233800
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD