Vinblastine sulfate salt 

Plant alkaloid that inhibits microtubule assembly by binding tubulin and inducing self-association in spiral aggregates in a reaction that appears to be regulated by the C-terminus of β-tubulin and is enhanced by GDP and GTP. Depolymerizes microtubules. Arrests the 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. Substrate of Pgp and CYP3A4.

≥96% (HPLC)

powder

white

267 °C (dec.)(lit.)

H₂O: 10 mg/mL

DMSO: 50 mg/mL

A1mM/214 nm, ethanol 53.7

A1mM/259 nm, ethanol 16.2

A1mM/270 nm, 0.1 M phosphate buffer 14

human ... TBCC(6903)

2-8°C

Jordan, M.A., and Wilson, L., Use of drugs to study role of microtubule assembly dynamics in living cells. Meth. Enzymol. 298, 252-276, (1998) abstract

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

Rai, S.S., and Wolff, J., The C terminus of β-tubulin regulates vinblastine-induced tubulin polymerization. Proc. Natl. Acad. Sci. USA 95, 4253-4257, (1998) 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

Panda, D., et al., Differential effects of vinblastine on polymerization and dynamics at opposite microtubule ends. J. Biol. Chem. 271, 29807-29812, (1996) 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

Chen, G.K., et al. Br. J. Cancer 83, 892-898, (2000) abstract

Zhou-Pan, X.R., er al. Cancer Res. 53, 5121-5126, (1993) abstract

Tishler, R.B., and Lamppu, D.M.,, The interaction of taxol and vinblastine with radiation induction of p53 and p21 WAF1/CIP1. Br. J. Cancer 74, S82-S85, (1996)

Tashiro, E., et al., Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells. Jpn. J. Jpn. J. Cancer Res. 89, 940-946, (1998) abstract

Merck 13,10044

Beil. 26,IV,3167

Aldrich MSDS 1, 1832:D / Corp MSDS 1 (2), 3598:B / IR-Spectra (3), 1511:H / RegBook 1 (2), 2883:I / Sax 6, 2725 / Sigma FT-IR 1 (1), 606:A / Structure Index 1, 461:A:7

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