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GNE-900

Chemical Structure : GNE-900

CAS No.: 1200126-26-6

GNE-900 (GNE 900;GNE900)

Catalog No.: PC-60310Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.
GNE-900 displays >300-fold selectivity over Aurora, PLK, CDK1/2) and ChK2.
GNE-900 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.
GNE-900 potentiates the efficacy of gemcitabine in tumor xenografts.

Physicochemical Properties

M.Wt 367.45
Formula C23H21N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Blackwood E, et al. Mol Cancer Ther. 2013 Oct;12(10):1968-80.

2. Xiao Y, et al. Mol Cancer Ther. 2013 Nov;12(11):2285-95.

3. Gazzard L, et al. J Med Chem. 2015 Jun 25;58(12):5053-74.

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