SAR020106
产品编号: DC9792
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应用领域
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.
| Cas No.: |
1184843-57-9 |
| 名称: |
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| 别名: |
SAR020106; SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106 |
| SMILES: |
C1(C2=C(C=C(N=C2)NC2C=NC(C#N)=C(O[C@@H](CN(C)C)C)N=2)C=CC=1)Cl |
| 分子式: |
C19H19ClN6O |
| 分子量: |
382.13 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility. |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_2801_DC9792_1184843-57-9 |
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COA
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DOWNLOAD |
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