Werner syndrome RecQ helicase-IN-4

Names

[ CAS No. ]:
2869954-53-8

[ Name ]:
Werner syndrome RecQ helicase-IN-4

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

[Target]

IC50: 0.06 µM (WRN)[1]


[In Vitro]

Werner syndrome RecQ helicase-IN-4 (example 58) (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 0.07，>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 0.07, >10 µM for SW48, DLD1 WRN-KO cells, respectively.

[In Vivo]

Werner syndrome RecQ helicase-IN-4 (240 mg/kg; daily for 18 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: 240 mg/kg Administration: P.o.; daily for 18 days Result: Inhibited tumor growth.

[References]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C32H33F3N8O5

[ Molecular Weight ]:
666.65

Related Compounds

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