Tretazicar

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CB1954(Tretazicar) 是一种抗癌前药，可被 NAD(P)H 醌氧化还原酶 2 激活。

Tretazicar (CB1954) is a dinitrobenzamide prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. CB1954 has been proposed for use in enzyme-prodrug gene therapy systems with the Escherichia coli enzyme nitroreductase (Ntr). Ntr converts CB1954 to 2- and 4-hydroxylamino derivatives, whereupon the non-enzymatic reaction of the 4-hydroxylamino derivative with cellular thio- esters generates a potent cytotoxic bifunctional alkylating agent capable of cross-linking DNA.

——

Animal Model:Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)Dosage:80 mg/kg Administration:i.p. on days 2 and 9 Result:The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.

CB1954 | CB-1954 | CB 1954 | Tretazicar

PI3K/Akt/mTOR signaling

mTOR

DNA alkylator

Cancer

——

21919-05-1

252.18

C9H8N4O5

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (495.68 mM)

NC(=O)c1c(cc(c(c1)N1CC1)[N+](=O)[O-])[N+](=O)[O-]

5-(aziridin-1-yl)-2,4-dinitrobenzamide

(-20℃)

With Ice Pack

≥ 2 years