Werner syndrome RecQ helicase-IN-4

• CAT Number: I041981
• CAS Number: 2869954-53-8
• Molecular Formula: C32H33F3N8O5
• Molecular Weight: 666.65
• Purity: ≥95%
• Synonyms: 2-[2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-6-[4-(3-hydroxypyridine-2-carbonyl)piperazin-1-yl]-7-oxo-[1,2,4]triazolo[1,5-a]pyrimidin-4-yl]-N-[2-methyl-4-(trifluoromethyl)phenyl]acetamide
• InChI: InChI=1S/C32H33F3N8O5/c1-3-23-27(40-11-13-41(14-12-40)29(46)26-24(44)5-4-10-36-26)30(47)43-31(38-28(39-43)20-8-15-48-16-9-20)42(23)18-25(45)37-22-7-6-21(17-19(22)2)32(33,34)35/h4-8,10,17,44H,3,9,11-16,18H2,1-2H3,(H,37,45)
• InChIKey: FLRLAYBOOSONEK-UHFFFAOYSA-N
• SMILES: CCC1=C(C(=O)N2C(=NC(=N2)C3=CCOCC3)N1CC(=O)NC4=C(C=C(C=C4)C(F)(F)F)C)N5CCN(CC5)C(=O)C6=C(C=CC=N6)O

Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity[1].
Werner syndrome RecQ helicase-IN-4 (example 58) (0-10 µM; 8-20 days) shows antiproliferative activity with GI50s of 0.07, >10 µM for SW48, DLD1 WRN-KO cells, respectively[1].
Werner syndrome RecQ helicase-IN-4 (240 mg/kg; daily for 18 days) shows anticancer activity in mouse[1].

Reference

[1]. Vincent Bordas, et al. Triazolo-pyrimidine analogues for treating diseases connected to the inhibiton of werner syndrome recq helicase (wrn). WO2022249060A1.