1188371-47-2

1188371-47-2 structure

Name: Valecobulin
Chemical 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
CAS Number: 1188371-47-2
Molecular Formula: C₂₆H₂₈N₆O₅S
Molecular Weight: 536.60300
Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
Create Date: 2017-04-30 06:31:36
Modify Date: 2024-01-23 00:04:46
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].

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
Synonyms	UNII-P48P97V001 CKD-516 free base

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	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin
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.