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(Vincaleukoblastine sulfate salt)
Vinblastine sulfate Chemical Structure
|Product name: Vinblastine sulfate|
|Cat. No.: HY-13780|
Vinblastine sulfate can inhibit the formation of microtubule, it also inhibit nAChR(IC50=8.9 uM).
IC50 Value: VIN showed EC50 values of 15 ug/ml, against P815 mastocytoma cells in-vitro. Also supresses nAChR activity with IC50 of 8.9 μM.
in vitro: At vinblastine concentrations of 0.5 uM and 2 uM, considerable inhibition of metabolic degradation of vinblastine was observed by competitive inhibitors of CYP3A4 (up to 60% inhibition), 2D6 (30%) and 2E1 (24%), while only a minor effect was observed for 2C9 (14%) and inhibitors of 1A2, 2C8 had no inhibitory effect on vinblastine metabolism. Vinblastine (0.5 and 2 uM) inhibited the metabolic capacity of CYP2C9 (up to 56%), 2C8 (36%), 2D6 (22%) and 3A4-mediated nifedipine oxidation (99%), while 3A4-mediated testosterone 6-beta-hydroxylation (max. 16%) as well as 1A2 and 2E1 remained unaffected.
in vivo: In combined intraperitoneal injection with vinblastine (200 micrograms kg-1) into P388/ADR-bearing mice, NA-382 in a suspension form (10 mg kg-1) prolonged the life-span of the mice near to that of P388/S-bearing mice treated with vinblastine alone, but verapamil even at the maximum tolerated dosage (30 mg kg-1) barely affected the in-vivo antitumour effect of vinblastine.
Clinical trial: Combination Chemotherapy With or Without Interleukin-2 and Interferon Alfa in Treating Patients With Metastatic Melanoma . Phase 3 Clinical
|M.Wt||909.05||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 44 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.1000 mL||5.5002 mL||11.0005 mL|
|5 mM||0.2200 mL||1.1000 mL||2.2001 mL|
|10 mM||0.1100 mL||0.5500 mL||1.1000 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Vinblastine sulfate||Cancer and Leukemia Group B||Hodgkins disease||30-SEP-10||31-MAY-15||Phase 2||09-OCT-13|
|St Jude Children's Research Hospital||Hodgkins disease||28-FEB-09||31-JUL-26||Phase 2||21-NOV-13|
|St Jude Children's Research Hospital||Acute lymphoblastic leukemia||31-OCT-12||31-OCT-19||Phase 2||22-OCT-13|
|Eastern Cooperative Oncology Group||Hodgkins disease||30-APR-12||01-JUN-21||Phase 2||14-SEP-13|
|Childrens Hospital of Philadelphia||Neurofibromatosis type I||28-FEB-01||Phase 2||10-SEP-13|
. Zhao C, Morgan M, Haeryfar SM, Exposure to paclitaxel or vinblastine down-regulates CD11a and CD54 expression by P815 mastocytoma cells and renders the tumor cells resistant to killing by nonspecific cytotoxic T lymphocytes induced with anti-CD3 antibody.
. MiyamotoK, TakedaK, KogaK,Antitumour effects and pharmacokinetics of combination of vinblastine with a staurosporine derivative, NA-382, inP388/ADR-bearing mice. J Pharm Pharmacol. 1995 Jun;47(6):524-9.
. Hilgendorf C, Doeppenschmitt S. In vitro metabolism of vinblastine: inhibition of CYP3A4 mediated nifedipine oxidation but not testosterone-6-beta hydroxylation. Eur.J.Clin.Pharmacol., 2001, 57, No. 8, A31
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