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Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC 50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity
In Vitro
Werner syndrome RecQ helicase-IN-3 (example 96) (0-10 µM; 8-20 days) shows antiproliferative activity with GI 50 s of 0.06, >10 µM for SW48, DLD1 WRN-KO cells, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: SW48, DLD1 WRN-KO cells Concentration: 0-10 µM Incubation Time: 8-20 days Result: Showed antiproliferative activity with GI 50 s of 0.06, >10 µM for SW48, DLD1 WRN-KO cells, respectively.
In Vivo
Werner syndrome RecQ helicase-IN-3 (120 mg/kg; daily for 22 days) shows anticancer activity in mouse . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Crl:NU(NCr)-Foxn1nu -Homozygous nude mice (SW48 xenografts cells) Dosage: 120 mg/kg Administration: P.o.; daily for 22 days Result: Inhibited tumor growth.
Form:Solid
IC50& Target:IC 50 : 0.06 µM (WRN)
| Canonical Smiles | O=C(N1CCN(CC1)C2=C(CC)N(CC(NC3=CC=C(C(F)(F)F)C=C3Cl)=O)C4=NC(C5=CCOCC5)=NN4C2=O)C6=NC=CC=C6O |
|---|---|
| Molecular Weight | 687.07 |
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