Vincristine sulfate salt 

Widely used in cancer research. In studies on multi-drug resistance.?; Inhibitor of monoamine oxidase B?

Plant alkaloid that inhibits microtubule assembly by binding tubulin and inducing coiled spiral aggregate formation. Arrests cell cycle in G2/M-phase by blocking mitotic spindle formation. Triggers Raf-1 activation, phosphorylation of bcl-2-family proteins, induction of p53 expression, and apoptosis in several tumor cell lines. Inhibits VEGF production in leukemia cell lines. Substrate for Pgp and CYP3A4. MRP1 transports vincristine in an ATP- and GSH-dependent manner.

95.0-105.0% (HPLC)

powder

≤12% ethanol(Actual content given on label.)

white or off-white

methanol: 20 mg/mL

−20°C

Lobert, S., et al., Interaction of vinca alkaloids with tubulin: a comparison of vinblastine, vincristine, and vinorelbine. Biochemistry 35, 6806-6814, (1996) abstract

Jordan, A., et al., Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med. Res. Rev. 18, 259-296, (1998) abstract

Poruchynsky, M.S., et al., Bcl-xL is phosphorylated in malignant cells following microtubule disruption. Cancer Res. 58, 3331-3338, (1998) abstract

Blagosklonny, M.V., et al., Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death. Cancer Res. 57, 130-135, (1997) abstract

Avramis, I.A., et al., Taxotere and vincristine inhibit the secretion of the angiogenesis inducing vascular endothelial growth factor (VEGF) by wild-type and drug-resistant human leukemia T-cell lines. Anticancer Res. 21, 2281-2286, (2001) abstract

Green, H., et al. Pharmacol. Toxicol. 93, 297-304, (2003) abstract

Jong-KeunSon, et al. J. Med. Chem. 33, 1845, (1990)

Horio, M., et al. Proc. Natl. Acad. Sci. USA 85, 3580, (1988)

Renes, J., et al. Br. J. Pharmacol. 126, 681-688, (1999) abstract

Murphy, J.A., et al. Lancet 346, 443, (1995) abstract

Bohme, A., et al., Ann. Hematol. Transition Metals for Organic Synthesis 71, 311-312, (1995)

Zelcer, N., et al. J. Biol. Chem. 276, 46400-46407, (2001) abstract

Mohammad, R.M., et al., Bryostatin 1 induces apoptosis and augments inhibitory effects of vincristine in human diffuse large cell lymphoma. Leuk. Res. 19, 667-673, (1995) abstract

Merck 13,10048

UN 2811 6.1/PG 2

3

OH6340000