AZD8330CAS号: 869357-68-6分子式: C16H17FIN3O4分子量: 461.23描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
AZD8330是一种新型,选择性的,非ATP竞争性MEK 1/2抑制剂,IC50为7 nM。AZD8330可以有效抑制MEK 1/2。在pERK系统中AZD8330能达到超豪微摩尔级的效力,在MEK 1/2抑制剂敏感的细胞系的功能(扩增)实验中也能达到低至超豪微摩尔级的效力。MEK抑制剂AZD8330特异性抑制促分裂原活化蛋白激酶激酶1(MEK 或 MAP/ERK激酶1),抑制了生长因子调节的细胞信号传导的过程并抑制了肿瘤细胞增殖。 |
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 |
ARRY-424704;ARRY-704
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可溶性/溶解性 |
Ethanol :85 mg/mL (184.3 mM)
DMSO :85 mg/mL (184.3 mM) |
生物活性 | |
靶点 |
ERK phosphorylation ,MEK1/2
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In vitro(体外研究) |
AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.
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In vivo(体内研究) |
In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily.
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分子结构图