GNE-900

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].

Product Specifications

CAS Number

[1200126-26-6]

UNSPSC

12352005

Target

Apoptosis; Checkpoint Kinase (Chk)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gne-900.html

Purity

99.21

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

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

Molecular Formula

C23H21N5

Molecular Weight

367.45

References & Citations

[1]Blackwood E, et al. Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900. Mol Cancer Ther. 2013 Oct;12 (10) :1968-80.