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

浓度为 1.25 nM 的Vinorelbine （0.5-5 nM）可抑制细胞增殖 50%（IC50）。浓度为 8 nM 的Vinorelbine 不会使细胞进入无丝分裂期[1]。Vinorelbine 在雄激素依赖型（AD）和独立型（AI）前列腺癌细胞系中具有时间依赖性，可诱导 p53 和 p21WAFI/CIP1 的表达。Vinorelbine 以浓度依赖性方式刺激报告基因[2]。

在接受Vinorelbine 治疗后，第一次中性粒细胞减少发生在第一次（4 只狗）、第二次（1 只）或第六次（1 只）Vinorelbine 治疗之后[3]。肿瘤猫对Vinorelbine 的耐受性为每周一次，MTD 为 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.