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/ MEK / Selumetinib/司美替尼

Selumetinib/司美替尼 {[allProObj[0].p_purity_real_show]}

货号：A351367 同义名： 司美替尼 (AZD6244) / AZD6244; ARRY-142886

Selumetinib(AZD6244) 是一种选择性、非ATP竞争性口服MEK1/2抑制剂，对MEK1的IC50为14 nM，并抑制ERK1/2的磷酸化。

Selumetinib/司美替尼 化学结构 CAS号：606143-52-6
Selumetinib/司美替尼 化学结构
CAS号：606143-52-6
Selumetinib/司美替尼 3D分子结构
CAS号：606143-52-6
Selumetinib/司美替尼 化学结构 CAS号：606143-52-6
Selumetinib/司美替尼 3D分子结构 CAS号：606143-52-6
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Selumetinib/司美替尼 纯度/质量文件 产品仅供科研

货号：A351367 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 MEK ↓ MEK1 ↓ MEK1/2 ↓ MEK2 ↓ MEK5 ↓ 其他靶点 纯度
Honokiol ✔ 98%
Mirdametinib ++++

MEK, IC50: 0.33 nM

 		99%+
Binimetinib +++

MEK, IC50: 12 nM

 		99%+
BI-847325 ++

MEK1, IC50: 25 nM

 		+++

MEK2, IC50: 4 nM

 		99%+
U0126-EtOH +

MEK1, IC50: 0.07 μM

 		++

MEK2, IC50: 0.06 μM

 		98%
GDC-0623 ++++

MEK1, IC50: 0.13 nM

 		99%+
TAK-733 ++++

MEK1, IC50: 3.2 nM

 		99%+
Trametinib ++++

MEK1, IC50: 0.92 nM

 		++++

MEK2, IC50: 1.8 nM

 		99%+
Selumetinib +++

MEK1, Kd: 99 nM

MEK1, IC50: 14 nM

 		+

MEK2, Kd: 530 nM

 		99%+
CI-1040 ++

MEK1, IC50: 17 nM

 		++

MEK2, IC50: 17 nM

 		99%+
Myricetin ✔ 98%
Refametinib ++

MEK1, IC50: 19 nM

 		++

MEK2, IC50: 47 nM

 		99%+
Cobimetinib +++

MEK1, IC50: 4.2 nM

 		99%+
PD98059 +

MEK1, IC50: 2 μM

 		99%+
SL327 +

MEK1, IC50: 0.18 μM

 		+

MEK2, IC50: 0.22 μM

 		AP-1 98+%
PD318088 ✔ 99%
AZD8330 +++

MEK1/2, IC50: 7 nM

 		99%+
Pimasertib 98%
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

 		99%+
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Selumetinib/司美替尼 生物活性

靶点

  • MEK2

    MEK2, Kd:530 nM

  • MEK1

    MEK1, Kd:99 nM

    MEK1, IC50:14 nM
描述 The Ras-Raf-MEK pathway is overactive in many human cancers, such as melanoma and NSCLC. Selumetinib, also called as ARRY-142886 or AZD6244, is a potent and highly selective MEK1/2 inhibitor with IC50 of 14 nM (measured by the catalytic activation of purified His-MEK1 on ERK2). Selumetinib can inhibit the enzymatic activity of MEK1/2 but not the MEK1/2 phosphorylation by Raf. IC50 of Selumetinib to inhibit MEK1/2 phosphorylation on ERK1/2 in cell lines examed is less than 40 nM. In EGFR-overexpressed A431 cells, EGF-induced ERK1/2 phosphorylation can be inhibited by Selumetinib at the concentration < 10 μM in a dose-dependent manner, while no obvious inhibition can be observed in ERK5. In cell growth study, Selumetinib shows more potent in cell lines containing activating B-Raf and Ras mutations (HT-29, Malme-3M, MIA PaCa-2, SK-MEL-2, SK-MEL-28 cells, IC50 values ranging from 59 to 473 nM), while it had no effect on other cell lines examined, including BxPC3, BT474 and Malme-3 cells with no Raf/Ras-mutantion reported. 21-day administration of selumetinib orally, BID, can inhibit the tumour growth up to 70% at the concentration of 100 mg/kg in mice bearing HT-29 tumors and inhibition of phospho-ERK1/2 was seen[1]. Selumetinib is mainly used in the study of melanoma, NSCLC, Neurofibromatosis type 1 etc.[2].
作用机制 Molecular modeling data shows Selumetinib can bind to the allosteric inhibitor binding site in MEK1/2[1].

Selumetinib/司美替尼 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
human A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=240.33 nM. SANGER
human A375 cells Proliferation assay 72 h Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=31 nM. 23474388
human A549 cell Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50=214.13 nM. SANGER
human AsPC-1 cell Growth inhibition assay Inhibition of human AsPC-1 cell growth in a cell viability assay, IC50=324.39 nM. SANGER

Selumetinib/司美替尼 动物研究

Dose Mice[3] (i.p.): min = 25 mg/kg, max = 100 mg/kg
Administration i.p.
Pharmacokinetics
Animal Nude mice[4]
Dose 10 mg/kg
Administration p.o.
Cmax 2977 ng/ml
T1/2 2.29 h
Tmax 1.0 h
AUC 17525 ng/(ml·h)
Vz/F 1.9 L/kg
Cl/F 0.6 L/(h·kg)

Selumetinib/司美替尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00085787 Advanced Cancer Phase 1 Completed - United States, Colorado ... 展开 >> University of Colorado Cancer Center, Anschutz Cancer Center Aurora, Colorado, United States, 80010 United States, Minnesota Mayo Clinic Rochester Rochester, Minnesota, United States, 55905 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT00780676 Breast Cancer Phase 2 Terminated(Closed early for fu... 展开 >>tility.) 收起 << - United States, Texas ... 展开 >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02546661 Muscle Invasive Bladder Cancer Phase 1 Recruiting March 27, 2020 -

Selumetinib/司美替尼 参考文献

[1]Yeh TC, Marsh V, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res. 2007 Mar 1;13(5):1576-83.

[2]Bernabé R, Patrao A, et al. Selumetinib in the treatment of non-small-cell lung cancer. Future Oncol. 2016 Nov;12(22):2545-2560.

[3]Bartholomeusz C, Oishi T, et al. MEK1/2 inhibitor selumetinib (AZD6244) inhibits growth of ovarian clear cell carcinoma in a PEA-15-dependent manner in a mouse xenograft model. Mol Cancer Ther. 2012 Feb;11(2):360-9.

[4]Denton CL, Gustafson DL, et al. Pharmacokinetics and pharmacodynamics of AZD6244 (ARRY-142886) in tumor-bearing nude mice. Cancer Chemother Pharmacol. 2011 Feb;67(2):349-60.

Selumetinib/司美替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.92mL

2.18mL

1.09mL

21.85mL

4.37mL

2.18mL

Selumetinib/司美替尼 技术信息

CAS号606143-52-6
分子式C17H15BrClFN4O3
分子量 457.68
SMILES Code O=C(C1=C(NC2=CC=C(Br)C=C2Cl)C(F)=C3N=CN(C)C3=C1)NOCCO
MDL No. MFCD11977472
别名 司美替尼 (AZD6244) ;AZD6244; ARRY-142886; ARRY886; NSC 741O78; CL 1,040
运输蓝冰
InChI Key CYOHGALHFOKKQC-UHFFFAOYSA-N
Pubchem ID 10127622
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 20 mg/mL(43.7 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
动物实验配方

4% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

Tags: Selumetinib | 606143-52-6 | AZD6244 | ARRY-142886 | AZD 6244 | AZD-6244 | ARRY142886 | ARRY 142886 | ARRY-142886 | MEK1/2 Inhibitor | MAPK/ERK Pathway | Apoptosis | MEK | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Selumetinib/司美替尼 纯度/质量文件 | Selumetinib/司美替尼 亚型比较 | Selumetinib/司美替尼 生物活性 | Selumetinib/司美替尼 细胞研究 | Selumetinib/司美替尼 动物研究 | Selumetinib/司美替尼 临床数据 | Selumetinib/司美替尼 参考文献 | Selumetinib/司美替尼 实验方案 | Selumetinib/司美替尼 技术信息

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