Vinrosidine
Vinrosidine (Leurosidine) is a mitotic spindle microtubule inhibitor with antitumor activity. Vinrosidine regulates tubulin dynamics at microtubule plus ends, disrupts mitotic spindle function, and blocks cell cycle progression at metaphase. Vinrosidine exhibits antitumor activity in multiple in vivo xenograft models. Vinrosidine can be used in cancer-related research.
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- No. CAS: 15228-71-4
- Fòrmula: C46H58N4O9
- Peso molecular:810.97
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
In Vitro
Vinrosidine (1000 nM-100 μM; 18-20 h) inhibits HeLa S3 cell proliferation by disrupting mitotic spindle function, causing metaphase arrest with a Ki,pol of 2200 nM, with 50% microtubule depolymerization occurring at a slightly higher concentration (2700 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vinrosidine (3.75 mg/kg; i.p.; once daily; for 10 consecutive days) prolongs the survival time of DBA/2 mice bearing P-1534 leukemia, and exhibits additive activity when used in combination with Vinleurosine (HY-120098) or Vincristine (HY-N0488A)[2].
Vinrosidine exhibits 100% tumor growth inhibition or >100% survival time prolongation against P-1534 leukemia and Ridgeway osteosarcoma; it shows moderate activity against Mecca lymphosarcoma, B82A leukemia, Ehrlich ascites, Freund ascites, S-180 ascites, and X-5568 myeloma in corresponding animal tumor models, but does not display detectable activity in a variety of other tumor models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2 mice (intraperitoneal inoculation of P-1534 leukemia cells)[2]
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Dosage:10 mg/kg; 7.5 mg/kg; 5.0 mg/kg; 4.0 mg/kg; 3.0 mg/kg; 2.0 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Produced 4 indefinite survivors with 1 toxic death at 10 mg/kg.
Produced 5 indefinite survivors at 7.5 mg/kg.
Prolonged survival time by 127% with no indefinite survivors at 5.0 mg/kg.
Prolonged survival time by 75% with no indefinite survivors at 4.0 mg/kg.
Prolonged survival time by 30% with no indefinite survivors at 3.0 mg/kg.
Prolonged survival time by 21% with no indefinite survivors at 2.0 mg/kg.
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Animal Model:DBA/2 mice (intraperitoneal inoculation of P-1534 leukemia cells)[2]
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Dosage:3.75 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Prolonged survival time by 37% with no indefinite survivors when administered alone.
Prolonged survival time by 128% with no indefinite survivors when combined with vinleurosine.
Prolonged survival time by 69% with 3 indefinite survivors when combined with vinblastine.
Prolonged survival time by 109% with 3 indefinite survivors when combined with vincristine.
Chemical Information
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No. CAS 15228-71-4
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Peso molecular 810.97
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Fòrmula C46H58N4O9
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SMILES
CC[C@@]12[C@@]3([H])[C@]4(CCN3CC=C2)[C@](N(C5=CC(OC)=C([C@@]6(C7=C(CC[N@@]8C[C@](C[C@@](O)(C8)CC)([H])C6)C9=CC=CC=C9N7)C(OC)=O)C=C54)C)([H])[C@](O)([C@@H]1OC(C)=O)C(OC)=O
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Synonyms
Leurosidine
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Vinrosidine Related Classifications
HY-126778 Related Classifications
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