ZYN57939

ZYN57939CAS号: 1639357-93-9分子式: C29H28N6O2S分子量: 524.62描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
ZYN57939 is RNA polymerase I inhibitor for treating RNA polymerase I- mediated diseases. ZYN57939 showed inhibitory activity with IC50 of 0.855 μM against human HT- 29 cancer cell lines.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
H2O:Insoluble,DMSO:5.25 mg/ml (10 mM)
生物活性
In vitro(体外研究)
MTR-106, stabilizes DNA G-quadruplexes in vitro.?MTR-106 displayed significant antiproliferative activity in homologous recombination repair (HR)-deficient and PARP inhibitor (PARPi)-resistant cancer cells.?Moreover, MTR-106 increased DNA damage and promoted cell cycle arrest and apoptosis to inhibit cell growth.
In vivo(体内研究)
MTR-106 oral and i.v. administration significantly impaired tumor growth in BRCA-deficient xenograft mouse models.?However, MTR-106 showed modest activity against talazoparib-resistant xenograft models.?In rats, the drug rapidly distributes to tissues within 5 min, and its average concentrations were 12-fold higher in the tissues than in the plasma.?Overall, MTR-106 as a novel G-quadruplex stabilizer with high tissue distribution, and it may serve as a potential anticancer agent.