TAS1553

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

TAS1553 是一种有效的口服活性蛋白-蛋白相互作用 (PPI) 抑制剂，其 IC50 值为 0.0396 μM。TAS1553 抑制 DNA 复制，减少细胞内 dATP 池。TAS1553 诱导细胞凋亡 (apoptosis)。TAS1553 可以用于癌症研究。

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.

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.Western Blot Analysis Cell Line:HCC38 and MV-4-11 cells Concentration:0, 0.1, 0.3, 1, 3 and 10 μM Incubation Time:0, 1, 2, 4, 8 and 24 hours Result:Increased the expression of Ser345, Ser4, Ser8 and Thr21 phosphorylation. Increaed the levels cleaved PARP and cleaved caspase-3.

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 24 hours 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.

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2166023-31-8

482.91

C20H20ClFN4O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (207.08 mM; 超声助溶 )

C[C@@H]([C@H](NS(=O)(=O)c1ccc(Cl)cc1C(N)=O)c1n[nH]c(=O)o1)c1c(F)ccc(C)c1C

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(-20℃)

With Ice Pack

≥ 2 years