Werner syndrome RecQ helicase-IN-3 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-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity[1].
Werner syndrome RecQ helicase-IN-3 (example 96) (0-10 µM; 8-20 days) 显示抗增殖活性，对 SW48，DLD1 WRN-KO 细胞的 GI50s 值分别为 0.06，>10 µM[1]。
Cell Proliferation Assay[1]
| Cell Line: | SW48, DLD1 WRN-KO cells |
| Concentration: | 0-10 µM |
| Incubation Time: | 8-20 days |
| Result: | Showed antiproliferative activity with GI50s of 0.06, >10 µM for SW48, DLD1 WRN-KO cells, respectively. |
Werner syndrome RecQ helicase-IN-3 (120 mg/kg; daily for 22 days) 在小鼠体内显示出抗癌活性[1]。
| Animal Model: | Female Crl:NU(NCr)-Foxn1nu -Homozygous nude mice (SW48 xenografts cells)[1] |
| Dosage: | 120 mg/kg |
| Administration: | P.o.; daily for 22 days |
| Result: | Inhibited tumor growth. |
[1]. Vincent Bordas, et al. Triazolo-pyrimidine analogues for treating diseases connected to the inhibiton of werner syndrome recq helicase (wrn). WO2022249060A1.