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Valecobulin

Chemical Structure : Valecobulin

CAS No.: 1188371-47-2

Valecobulin (CKD-51, CKD516)

Catalog No.: PC-35472Not For Human Use, Lab Use Only.

CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo.

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Biological Activity

CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo.
CKD-516 demonstrates potent cytotoxicity against several cancer cells including P-gp overexpressing MDR positive cell line (HCT15), also induces cell cycle arrest at G(2)/M phase, which is associated with strong inhibition of tubulin polymerization.
CKD-516 shows antitumor efficacy against both murine tumors (CT26 and 3LL) and human xenogratfs (HCT116 and HCT15) in mice.

Physicochemical Properties

M.Wt 536.607
Formula C26H28N6O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-2-amino-3-methyl-N-{4-[3-(1H-1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl]-1,3-thiazol-2-yl}butanamide

References

1. Lee J, et al. J Med Chem. 2010 Sep 9;53(17):6337-54.

2. Kim KW, et al. Invest New Drugs. 2013 Oct;31(5):1097-106.

3. Lee J, et al. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6327-30.

4. Kim YI, et al. Anticancer Res. 2014 Apr;34(4):1715-22.

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