Chemical Structure : GNE-900
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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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.
M.Wt | 367.45 | |
Formula | C23H21N5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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