GNE-900

Research use only, not for human use.

GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.

GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM; displays >300-fold selectivity over Aurora, PLK, CDK1/2) and ChK2; abrogates DNA damage-induced S and G2–M checkpoints (EC50=61.8 nM in H-29 cells), and exacerbates DNA double-strand breaks (DSB) to induce cell death, accelerates the demise of damaged HCT-116 colorectal cancer cells in a p53-dependent manner in vitro; potentiates the efficacy of gemcitabine in tumor xenografts.

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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.

GNE 900 | GNE900

Angiogenesis

Chk

Chk

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1200126-26-6

367.45

C23H21N5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (272.15 mM)

N#CC1=NC=C2C(C3=CC(C4=CC=C(CN5CCCCC5)C=C4)=CN=C3N2)=C1

3-(4-(piperidin-1-ylmethyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years