Vinorelbine (KW-2307 base) is a semisynthetic vinca alkaloid. Vinorelbine binds to tubulin and prevents the formation of the mitotic spindle, resulting in the arrest of tumor cell growth in metaphase.

Proliferation (Hela cells):1.25 nM

Vinorelbine (0.5-5 nM) inhibits cell proliferation by 50% (IC50) at 1.25 nM, with no cells in anaphase at 8 nM[1]. It time-dependently induces p53 and p21WAF1/CIP1 expression in androgen-dependent (AD) and -independent (AI) prostate cancer cell lines and stimulates reporter genes in a concentration-dependent manner[2].

After vinorelbine treatment, the initial neutropenic episode occurred after the first administration in four dogs, the second in one dog, and the sixth in another dog [3]. In tumor-bearing cats, vinorelbine is tolerated at a weekly interval with a maximum tolerated dose (MTD) of 11.5 mg/m2 [4].

Reverse transcriptase assays: Reverse transcriptase assays are carried out in a reaction mixture (50 μL) containing 50 mM Tris-HCl (pH 7.5), 5 mM DTT, 100 mM potassium chloride, 0.01% Triton X-100 or NP40, 10 μg/ml (dT)15.(A)n as template primer and [3H] deoxythymidine triphospahate. The reaction mixture is incubated for 1 hr at 37 ℃ and stopped by the addition of 50 μg of yeast tRNA and 2 mL of 10% solution of trichloroacetic acid containing 1 mM sodium pyrophosphate. The samples are filtered on filters (0.45 μm), washed first with 5% TCA solution for 5 times and then with 2 ml of 70% ethanol. The filters are dried, scintillation fluid is added and the radioactivity counted in a counter.