ZYN57939 是用于治疗 RNA 聚合酶 I 介导的疾病的 RNA 聚合酶 I 抑制剂。 ZYN57939 对人 HT-29 癌细胞系显示出抑制活性，IC50 为 0.855 μM。

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.

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.

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.

1639357-93-9

C29H28N6O2S

524.64

MTR-106

DMSO:5.25 mg/ml (10 mM),Need ultrasonic
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years