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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
AZD6244; ARRY-142886
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
606143-52-6
- 规格：
10 mM * 1 mL/50 mg/100 mg/200 mg/500 mg/1 g
| 规格： | 10 mM * 1 mL | 产品价格： | ￥790.0 |
|---|---|---|---|
| 规格： | 50 mg | 产品价格： | ￥600.0 |
| 规格： | 100 mg | 产品价格： | ￥958.0 |
| 规格： | 200 mg | 产品价格： | ￥1300.0 |
| 规格： | 500 mg | 产品价格： | ￥2600.0 |
| 规格： | 1 g | 产品价格： | ￥4500.0 |
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Selumetinib
CAS No. : 606143-52-6
MCE 国际站：Selumetinib
产品活性：Selumetinib (AZD6244) 是一种高效选择性的，非 ATP 竞争性的 MEK1/2 抑制剂， 抑制 MEK1 的 IC50 为14 nM。Selumetinib (AZD6244) 抑制 MEK1/2 磷酸化水平。
研究领域：MAPK/ERK Pathway | Apoptosis
In Vitro: Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells.
Selumetinib (AZD6244) (1μM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells.
Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line.
In Vivo: Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model.
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文献和实验免疫治疗的新策略。9. 与临床试验并行的 GEM 模型最近推出的 “与临床共试验” 范例，目的是将临床前 GEM 实验与人体临床试验同时开展，从而达到预测治疗效果的作用。该策略已经应用于前列腺癌治疗中，并成功揭示了由雄性激素诱发的耐受性是其中遗传关键因子，以及在克服去势难治性的新综合疗法。同样，应用 NSCLC 的 GEM 模型一起临床试验表明，Kras/Lkb1 突变肺癌较 Kras or Kras/p53 突变肿瘤对临床上的 Docetaxel 和 MEK 抑制剂 Selumetinib 的联合疗法，表现
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