Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
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.
Download
Download Datasheet