Vincristine Sulfate

DescriptionVincristine sulfate (2068-78-2) arrests cell cycle at G2/M by interfering with mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins.1,2Induces apoptosis.3Vincristine sulfate is a clinically useful cancer chemotherapeutic agent.

UsesVincristin sulfate USP (Oncovin) is used to treat acute leukemia in children; lymphocytic leukemia; Hodgkin’s disease; non-Hodgkin’s lymphomas; Wilm’s tumor; neuroblastoma; rhabdomyosarcoma.

UsesAn antitumor alkaloid isolated from Vinca rosea Linn. An antineoplastic.

UsesH1-antihistamine

UsesVincristine sulfate, is used as an anticancer agent, microtubule disrupter, Induces apoptosis in human lymphoma cells. Other applications include as a cell cycle arresting, apoptotic inducing alkaloid.

General DescriptionVincristine sulfate appears as an anticancer drug. White to slightly yellow, amorphous or crystalline powder. Sensitive to light. Odorless. pH (0.1% solution) 3.5 - 4.5. (NTP, 1992)

Preparation2g of vincristine sulfate was dissolved in 240ml of tetrahydrofuran, and 7.5ml of glacial acetic acid was added. Under its protection, the mixture was cooled to -65℃ with dry ice. While stirring, a prepared sodium dicadmium dicadmium solution (3g of sodium dicadmium dicadmium dissolved in 15ml of water, then 2ml of concentrated sulfuric acid was added and stirred until dissolved) was added dropwise, maintaining the reaction temperature below -50℃ during the addition. After the addition was complete, the reaction was stirred at -65℃ for 3 hours. The reaction solution was poured into a mixture of 35ml of concentrated ammonia and 200ml of water, extracted with 600ml of dichloromethane, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to obtain 2.06g of crude vincristine, with a purity of 83% as determined by HPLC. The crude vincristine was dissolved in 20 ml of isopropanol. While stirring, 16 ml of 1% isopropanol sulfate solution was added dropwise to adjust the pH to ≤ 4. The solid was filtered off, dried under vacuum, and 1.82 g of crude vincristine sulfate was obtained, with a purity of 92% as determined by HPLC. 1.8 g of crude vincristine sulfate was dissolved in 36 ml of anhydrous ethanol, cooled to -10°C, and stirred slowly. A solid precipitated, was filtered, washed with anhydrous ethanol, and dried under vacuum, yielding 1.63 g of vincristine sulfate, with a yield of 81.5% and a purity of 98.6% as determined by HPLC.