About: Tubulin Polymerization Inhibitor CKD-516     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Tubulin Polymerization Inhibitor CKD-516
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Tubulin Polymerization Inhibitor CKD-516
UMLS_CUI
  • C2974542
PDQ_Open_Trial_Search_ID
  • 729699
PDQ_Closed_Trial_Search_ID
  • 729699
FULL_SYN
  • CKD-516CNNCI
  • Tubulin Polymerization Inhibitor CKD-516PTNCI
  • (S)-N-(4-(3-(1H-1,2,4-Triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl)thiazol-2-yl)-2-amino-3-methylbutanamide HydrochlorideSNNCI
DEFINITION
  • A benzophenone derivative and water soluble valine prodrug of the tubulin binding agent S516, with potential tubulin-inhibiting, vascular-disrupting and antineoplastic activity. Upon administration, tubulin polymerization inhibitor CKD-516 is converted into its active metabolite S-516 that binds to tubulin and prevents its polymerization in tumor blood vessel endothelial cells and tumor cells. This blocks the formation of the mitotic spindle and leads to cell cycle arrest at the G2/M phase. As a result, this agent disrupts the tumor vasculature and tumor blood flow, deprives tumor cells of nutrients and induces tumor cell apoptosis. In addition, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization.NCI
code
  • C101264
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