Valecobulin

Modify Date: 2024-01-23 00:04:46

Valecobulin Structure
Valecobulin structure
Common Name Valecobulin
CAS Number 1188371-47-2 Molecular Weight 536.60300
Density N/A Boiling Point N/A
Molecular Formula C26H28N6O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Valecobulin


Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-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
Synonym More Synonyms

 Valecobulin Biological Activity

Description Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
Related Catalog
Target

Beta-tubulin polymerization[1].

In Vivo The size change of the tumor in VX2 liver tumor-bearing rabbits is significantly smaller in the Valecobulin (CKD516)( 5, 9, or 12 mg/m2, i.v.)- treated group than in control group[2]. Animal Model: VX2 liver tumor-bearing rabbits (Male New Zealand White rabbits weighing between 2.5 and 3.5 kg)[2]. Dosage: Dissolved in 5 mL of saline at a dose of 5, 9, or 12 mg/m2 of body surface area. Administration: Intravenous injection once. Result: The size change of the tumors was significantly smaller in the treated group than in control group.
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 C26H28N6O5S
Molecular Weight 536.60300
Exact Mass 536.18400
PSA 175.21000
LogP 4.91920

 Synonyms

UNII-P48P97V001
CKD-516 free base
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