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CKD-516

CAS No. 1188371-47-2

CKD-516( Valecobulin | CKD516 )

Catalog No. M10645 CAS No. 1188371-47-2

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CKD-516
  • Note
    Research use only, not for human use.
  • Brief Description
    CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo.
  • Description
    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.
  • In Vitro
    ——
  • 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. Animal Model:Male BALB/C nu/nu mice (5-6 weeks of age) with HCT-116 or HCT-15 cells 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.
  • Synonyms
    Valecobulin | CKD516
  • Pathway
    Cytoskeleton/Cell Adhesion Molecules
  • Target
    Microtubule/Tubulin
  • Recptor
    Microtubule/Tubulin
  • Research Area
    Cancer
  • Indication
    Colon Cancer

Chemical Information

  • CAS Number
    1188371-47-2
  • Formula Weight
    536.607
  • Molecular Formula
    C26H28N6O5S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (232.95 mM)
  • SMILES
    CC(C)[C@H](N)C(NC1=NC(C2=CC=C(C(C3=CC(OC)=C(OC)C(OC)=C3)=O)C(N4N=CN=C4)=C2)=CS1)=O
  • Chemical Name
    (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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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