TAS1553

• CAT Number: I043309
• CAS Number: 2166023-31-8
• Molecular Formula: C20H20ClFN4O5S
• Molecular Weight: 482.91
• Purity: ≥95%
• Synonyms: 5-chloro-2-[[(1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(2-oxo-3H-1,3,4-oxadiazol-5-yl)propyl]sulfamoyl]benzamide
• InChI: InChI=1S/C20H20ClFN4O5S/c1-9-4-6-14(22)16(10(9)2)11(3)17(19-24-25-20(28)31-19)26-32(29,30)15-7-5-12(21)8-13(15)18(23)27/h4-8,11,17,26H,1-3H3,(H2,23,27)(H,25,28)/t11-,17+/m1/s1
• InChIKey: DUYRWEBTZNUILI-DIFFPNOSSA-N
• SMILES: CC1=C(C(=C(C=C1)F)C(C)C(C2=NNC(=O)O2)NS(=O)(=O)C3=C(C=C(C=C3)Cl)C(=O)N)C

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[1].
TAS1553 (0.001-1 μM) inhibits the enzymatic activity of RNR in a dose-dependent manner[1].
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[1].
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[1].
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[1].
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[1].
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[1].

Reference

[1]. Ueno H, et, al. TAS1553, a small molecule subunit interaction inhibitor of ribonucleotide reductase, exhibits antitumor activity by causing DNA replication stress. Commun Biol. 2022 Jun 9;5(1):571.
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