| Identification | Back Directory | [Name]
CKD-516 (hydrochloride) | [CAS]
1240321-53-2 | [Synonyms]
CKD-516 HCl
UNII-2J9QE0TM5I
CKD-516 (hydrochloride)
(2S)-2-amino-3-methyl-N-[4-[3-(1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl]-1,3-thiazol-2-yl]butanamide:hydrochloride
Valecobulin hydrochloride,antitumor,β-tubulin,Inhibitor,Valecobulin,Microtubule/Tubulin,inhibit,prodrug,S516,CKD 516,VDA,CKD-516,CKD516 | [Molecular Formula]
C26H29ClN6O5S | [MOL File]
1240321-53-2.mol | [Molecular Weight]
573.07 |
| Hazard Information | Back Directory | [Uses]
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine proagent of S516 (HY-130233) 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]. | [in vivo]
Valecobulin (5 mg/kg; intraperitoneal injection; administered on days 2, 6, 10, and 14; male BALB/C nu/nu mice) treatment shows markedly antitumor efficacy in various human tumor xenograft models[1]. | Animal Model: | Male BALB/C nu/nu mice (5-6 weeks of age) with HCT-116 or HCT-15 cells[1] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; administered on days 2, 6, 10, and 14 | | Result: | Had shown marked antitumor efficacy in various human tumor xenograft models.
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| [References]
[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. DOI:10.1021/jm1002414
[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. DOI:10.1148/radiol.14131165 |
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