Cyanotriazole CT3

Chemical Structure : Cyanotriazole CT3

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货号: PC-20947Not For Human Use, Lab Use Only.

Cyanotriazole CT3 is a potent, selective, irreversible inhibitor of trypanosomal topoisomerase II, shows potent trypanocidal activity both in vitro and in vivo.

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生物&药学活性

Cyanotriazole CT3 is a potent, selective, irreversible inhibitor of trypanosomal topoisomerase II, shows potent trypanocidal activity both in vitro and in vivo.
Cyanotriazole CT3 is a potent growth inhibitor of a panel of kinetoplastid parasites, which includes T. cruzi and L. donovani (EC50, 78 and 134 nM), but has no activity against a range of nontrypanosomatid microbial pathogens.
Cyanotriazole CT3 (30 mg/kg) is efficacious against trypanosomatid parasites in vivo.
Cyanotriazole CT3-treated parasites showes defects in nuclear DNA replication, exhibited up-regulated DNA damage response.
Cyanotriazole CT3 selectively inhibits the DNA relaxation activity of trypanosome TopoII by stabilizing the dsDNA:enzyme complex, interacts covalently with C477 and bind at the DNA cleavage site.

物理化学性质&存储条件

分子量	416.34
分子式	C19H12F4N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N#CC1=NN(CC(N2CC3=C(C=C(C4=CC(F)=CN=C4C(F)(F)F)C=C3)C2)=O)C=N1

参考文献

1. Srinivasa P S Rao, et al. Science. 2023 Jun 30;380(6652):1349-1356.