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CB30865

Cat No.
CEI-1266
Product Overview
TS CB30865 is a highly potent cytotoxic agent. The compound inhibits isolated mammalian thymidylate synthase (TS), but this inhibition is insufficient to account for its cellular toxicity. Thymidylate synthase (TS) is a critical enzyme in the de novo synthesis of thymidylate (dTTP) and has long been recognized as a target for chemotherapeutic intervention.
CAS No.
206275-15-2
Molecular Weight
516.39
Purity
0.98
Storage
Store at -20°C
Synonyms
ZM242421; CB-30865; CB 30865; ZM-242421; ZM 242421
Targets
Nampt
IC50
2.8 nM for W1L2; 156 nM for isolated mammalian
Molecular Formula
C26H22BrN5O2
Chemical Name
4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
CB30865 was the most potent growth inhibitory agent (IC50 values in the range 1-100 nM for several mouse and human cell types). Against W1L2 cells, the analogues of CB300179 and CB300189 demonstrated reduced potency in the presence of exogenous thymidine (dThd), and against a W1L2:C1 TS overproducing cell line. In contrast, CB30865 retained activity in these systems. No cell cycle redistribution was observed following exposure (4-48 h) to an equitoxic concentration of CB30865.
In vivo
The in vivo evaluation of CB30865 was hampered because of its low aqueous solubility.
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