Valecobulin (CKD-516) (CKD516) 是 (S516) 的缬氨酸前药和血管破坏剂 (VDA)。 Valecobulin (CKD-516) 是一种有效的 β-tubulin 聚合抑制剂,对小鼠和人类实体瘤具有显着的抗肿瘤活性。
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Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
The size change of the tumor in VX2 liver tumor-bearing rabbits is significantly smaller in the Valecobulin (CKD516)( 5, 9, or 12 mg/m2, i.v.)- treated group than in control group[2].|| Animal Model:|VX2 liver tumor-bearing rabbits (Male New Zealand White rabbits weighing between 2.5 and 3.5 kg)[2]. |Dosage:|Dissolved in 5 mL of saline at a dose of 5, 9, or 12 mg/m2 of body surface area.|Administration:|Intravenous injection once.|Result:|The size change of the tumors was significantly smaller in the treated group than in control group.
[1]. Lee J, et al. Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors. J Med Chem. 2010 Sep 9;53(17):6337-54. [2]. Joo I, et al. Intravoxel incoherent motion diffusion-weighted MR imaging for monitoring the therapeutic efficacy of the vascular disrupting agent CKD-516 in rabbit VX2 liver tumors. Radiology. 2014 Aug;272(2):417-26.
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