Werner syndrome RecQ helicase-IN-4

Modify Date: 2024-01-18 18:54:25

Werner syndrome RecQ helicase-IN-4 Structure
Werner syndrome RecQ helicase-IN-4 structure
Common Name Werner syndrome RecQ helicase-IN-4
CAS Number 2869954-53-8 Molecular Weight 666.65
Density N/A Boiling Point N/A
Molecular Formula C32H33F3N8O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Werner syndrome RecQ helicase-IN-4


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].

 Names

Name Werner syndrome RecQ helicase-IN-4

 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
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