TH1217 是一种有效的、选择性的 dCTPase pyroPhosphatase 1 (dCTPase) 抑制剂，IC50 值为 47 nM。TH1217 可增强胞苷类似物在白血病细胞中的细胞毒性作用。TH1217 还可以调节 SARS-Cov-2 相互作用体，因此它具有抗 COVID-19 的活性。
产品描述
TH1217 is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
体外活性
TH1217 (compound 30) inhibits dCTPase and enhances aqueous solubility (>100 μM) and improves plasma stability in vitro(t4h=86%). TH1217 presents suitable mouse microsomal half-lives (109 minutes). TH1217 displays well cell permeability (8.66×10-6/1.30×10-3 cm/s) and CYP inhibition[1].
Cas No.
1862212-48-3
分子式
C20H17BCl2N4O6
分子量
491.09
别名
TH 1217
储存和溶解度
DMSO:117mg/mL (238.2mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
