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CKD-516

Chemical Structure : CKD-516

CAS No.: 1188371-47-2

CKD-516 (Valecobulin;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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo; 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; shows antitumor efficacy against both murine tumors (CT26 and 3LL) and human xenogratfs (HCT116 and HCT15) in mice.

Colon Cancer

Phase 2 Clinical

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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