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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-GNE-900
GNE-900

Chemical Structure : GNE-900

CAS No.: 1200126-26-6

GNE-900 (GNE 900;GNE900)

货号: 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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10 mg ¥3180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 367.45
分子式 C23H21N5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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