AZD-3759CAS号： 1626387-80-1分子式： C22H23ClFN5O3分子量： 459.90描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity.
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| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
AZD-3759,AZD 3759,,AZD3759
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| 外观 |
Powder
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| 可溶性/溶解性 |
DMSO 92 mg/mL (200.04 mM)
Ethanol 44 mg/mL warmed (95.67 mM) |
| 生物活性 | |
| 靶点 |
EGFR (L858R) ,EGFR (exon 19Del) ,EGFR (WT)
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| In vitro(体外研究) |
In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells.
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| In vivo(体内研究) |
AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy.
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分子结构图
