| Identification | Back Directory | [Name]
CKD-516 | [CAS]
1188371-47-2 | [Synonyms]
CKD-516
Valecobulin
(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
Butanamide, 2-amino-3-methyl-N-[4-[3-(1H-1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl]-2-thiazolyl]-, (2S)- | [Molecular Formula]
C26H28N6O5S | [MDL Number]
MFCD25976612 | [MOL File]
1188371-47-2.mol | [Molecular Weight]
536.6 |
| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (232.95 mM) | [form ]
Solid | [pka]
6.43±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Valecobulin (CKD516) is a valine proagent of (S516) and a vascular disrupting agent (VDA). Valecobulin 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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| [storage]
Store at -20°C | [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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