Selumetinib sulfate|943332-08-9|-陌孚医药/Medlife

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Selumetinib sulfate

目录号: PL07040 纯度: ≥99%

CAS No. :943332-08-9

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中文名称	Selumetinib sulfate
中文别名	[司美替尼盐]
英文名称	Selumetinib sulfate
英文别名	6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide,sulfuric acid;Selumetinib sulfate;Selumetinib (sulfate);AZD6244 HYD-SULFATE;807ME4B7IJ;AZD6244 HYDROGEN SULFATE;6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide;sulfuric acid;Selumetinib sulfate [USAN];Koselugo (TN);AZD6244 Hyd-Sulf;Selumetinib sulfate (JAN/USAN);NSC748727;Z;AZD6244 sulfate;ARRY-142886 sulfate;AZD 6244 hyd-sulfate;AZD 6244 hydrogen sulfate;AZD-6244 hydrogen sulfate;AZD6244 hydrogen sulfate
Cas No.	943332-08-9
分子式	C₁₇H₁₇BrClFN₄O₇S
分子量	555.76
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC 50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

性状

Solid

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. [1].Huynh H, et al, Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Therapy, 2007, 6 (1), 138-146
[2]. [2].Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994.

溶解度数据	In Vitro: DMSO : 50 mg/mL (89.97 mM; Need ultrasonic)H₂O : 1 mg/mL (1.80 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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