Valecobulin hydrochloride (CKD-516 hydrochloride) 是 S516 的缬氨酸前体药和血管阻断剂 (VDA), 是一种强效的、β-微管蛋白聚合抑制剂，对小鼠和人类的实体肿瘤具有显著的抗肿瘤活性。
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
[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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