产品
编 号:F741395
分子式:C20H20ClFN4O5S
分子量:482.91
产品类型
结构图
CAS No: 2166023-31-8
联系客服
产品详情
生物活性:
TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.
体内研究:
TAS1553 (25-200 mg/kg; p.o.; for 24 h; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) has RNR inhibition effect in vivo.TAS1553 (50-200 mg/kg; p.o.; daily, for 15 d; female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice) has antitumor activity in vivo.Animal Model:Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice
Dosage:25, 50, 100 and 200 mg/kg
Administration:Oral administration; for 24hours
Result:Reduces intracellular dATP pool and induces the replication stress and apoptosis.
Animal Model:Female F344/NJcl-rnu/rnu rats and BALB/cAJcl-nu/nu mice
Dosage:50, 100 and 200 mg/kg
Administration:Oral administration; daily, for 15 days
Result:Inhibited tumor growth in the treated group/control group (T/C) were 52.0 (50 mg/kg), 45.0 (100 mg/kg) and 29.4% (200 mg/kg), respectively.
体外研究:
TAS1553 (0.001-1 μM) inhibits the enzymatic activity of RNR in a dose-dependent manner.TAS1553 (3 d) has anti-proliferative activity against both solid and hematological human cancer cell lines and the GI50 values ranged from 0.228 to 4.15?μM.TAS1553 (1-10 μM; 0-2 h; HCC38 and MV-4-11 cells) reduces intracellular dATP pool in a dose- and time-dependent manner, which is a critical metabolite for DNA replication.TAS1553 (0-10 μM; 0-24 h; HCC38 and MV-4-11 cells) induces the replication stress and apoptosis in a dose- and time-dependent manner.