GNE-900

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC 50 s of 0.0011, 1.5 µM for ChKl, ChK2 , respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis . gemcitabine and GNE-900 administration shows anti-tumor activity In Vitro GNE-900 (1 µM; 1-48 h) induces apoptosis with increases in the expression of cleaved PARP when combined with gemcitabine (50 nM) in HT-29 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: HT-29 cells Concentration: 1 µM Incubation Time: 1-48 h Result: Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM). In Vivo GNE-900 (2.5-40 mg/kg; p.o.; once) decreases the tumor volume and increases DNA damage, γ-H2AX levels when combinated with gemcitabine in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats (HT-29 tumor xenografts) Dosage: 2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg) Administration: P.o.; once Result: Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels. IC50& Target:Chk1 0.0011 μM (IC 50 ) Chk2 1.5 μM (IC 50 )

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