CKD-516

Research use only, not for human use.

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

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.

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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.

Valecobulin | CKD516

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Microtubule/Tubulin

Cancer

Colon Cancer

1188371-47-2

536.607

C26H28N6O5S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (232.95 mM)

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

(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

(-20℃)

With Ice Pack

≥ 2 years