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Vinblastine Chemical Structure
|Product name: Vinblastine|
|Cat. No.: HY-17418|
Vinblastine 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||810.97||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 42 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.2331 mL||6.1655 mL||12.3309 mL|
|5 mM||0.2466 mL||1.2331 mL||2.4662 mL|
|10 mM||0.1233 mL||0.6165 mL||1.2331 mL|
. 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
CAS No.: 143-67-9 In-stock
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