CKD-516

Modify Date: 2025-08-30 12:59:27

CKD-516 Structure
CKD-516 structure
Common Name CKD-516
CAS Number 1240321-53-2 Molecular Weight 573.06400
Density N/A Boiling Point N/A
Molecular Formula C26H29ClN6O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CKD-516


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].

 Names

Name (2S)-2-amino-3-methyl-N-[4-[3-(1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl]-1,3-thiazol-2-yl]butanamide,hydrochloride
Synonym More Synonyms

 CKD-516 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

[1]. Lee J, et al. Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors. J Med Chem. 2010 Sep 9;53(17):6337-54.

[2]. Joo I, et al. Intravoxel incoherent motion diffusion-weighted MR imaging for monitoring the therapeutic efficacy of the vascular disrupting agent CKD-516 in rabbit VX2 liver tumors. Radiology. 2014 Aug;272(2):417-26.

 Chemical & Physical Properties

Molecular Formula C26H29ClN6O5S
Molecular Weight 573.06400
Exact Mass 572.16100
PSA 175.21000
LogP 5.72120

 Synonyms

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
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