AZD6244 (Selumetinib).|606143-52-6|(司美替尼; AZD6244; ARRY-142886)-陌孚医药/Medlife

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AZD6244 (Selumetinib). (Synonyms: 司美替尼; AZD6244; ARRY-142886)

目录号: PC11765 纯度: ≥98%

CAS No. :606143-52-6

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中文名称

AZD6244 (Selumetinib).

中文别名

司美替尼;5-[(4-溴-2-氯苯基)氨基]-4-氟-N-(2-羟基乙氧基)-1-甲基-1H-苯并咪唑-6-甲酰胺;5-[(4-溴-2-氯苯基)氨基]-4-氟-N-(2- 羟基乙氧基)-1-甲基-1H-苯并咪唑-6-羧胺;AZD6244粉末;AZD6244固体状;AZD6244司美替尼;Selumetinib (AZD6244) 抑制剂;科研实验AZD6244;临床实验AZD6244;司美替尼SelumetinibAZD6244;司美替尼产品使用说明书及注意事项;医药级AZD6244;3-氧杂-9-氮杂螺[5.5]十一烷盐酸盐;5-[(4-溴-2-氯苯基)氨基]-4-氟-N-(2-羟基乙氧基)-1-甲基-1H-苯并[D]咪唑-6-甲酰胺

英文名称

AZD6244 (Selumetinib)

英文别名

AZD 6244;5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide;Selumetinib;Selumetinib (AZD6244);1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2- hydroxyethoxy)-1-methyl-;5-(4-bromo-2-chlorophenylamino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-c...;6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide;AZD-6244;AZD6244 (Selumetinib);Name: AZD 6244;SeluMetinib (AZD-6244);Selumetinib(AZD6244,ARRY-142886);6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide;Array142886;ARRY 142886;ARRY-142886;AZD6244;AZD6244(Selumetinib);5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide;5-(4-broMo-2-chlorophenylaMino)-4-fluoro-N-(2-hydroxyethoxy)-1-Methyl-1H-benzo[d]iMidazole-6-carboxaMide

Cas No.

606143-52-6

分子式

C₁₇H₁₅BrClFN₄O₃

分子量

457.68

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

性状

Solid

IC50 & Target[1][2]

MEK

12 nM (IC₅₀)

MEK1

14 nM (IC₅₀)

MEK2

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.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

Solvent&Solubility

DMF: 15 mg/ml
DMSO: 20 mg/ml
DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml

描述&特点

MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.1 AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).2,3,1 It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.2 AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.3,1 In addition to suppressing growth, it induces apoptosis and differentiation within tumors.4 AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.5,6

参考文献

[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 [Information]

[2]. Garon EB, et al. Identification of common predictive markers of 体外研究 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. [Information]

[3]. Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res, 2007, 13 (5), 1576-1583. [Information]

[4]. Sebolt-Leopold JS, et al. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer. 2004 Dec;4(12):937-47. [Information]

[5]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116. [Information]

[6]. Weisberg E, et al. Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clin Cancer Res. 2014 Nov 1;20(21):5483-95. [Information]

溶解度数据

体外研究:

DMSO : 10 mg/mL (21.85 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1849 mL	10.9247 mL	21.8493 mL
5 mM	0.4370 mL	2.1849 mL	4.3699 mL
10 mM	0.2185 mL	1.0925 mL	2.1849 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1 mg/mL (2.18 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

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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