CKD-516
Names
[ CAS No. ]:
1240321-53-2
[ Name ]:
CKD-516
[Synonym ]:
CKD-516
UNII-2J9QE0TM5I
(S)-N-(4-(3-(1H-1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl)thiazol-2-yl)-2-amino-3-methylbutanamide hydrochloride
Biological Activity
[Description]:
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
[Related Catalog]:
[Target]
β-tubulin polymerization[1]
[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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C26H29ClN6O5S
[ Molecular Weight ]:
573.06400
[ Exact Mass ]:
572.16100
[ PSA ]:
175.21000
[ LogP ]:
5.72120