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AZD8330 (Synonyms: ARRY-424704; ARRY-704; AZD-8330; ARRY424704; ARRY704; AZD8330)

カタログ番号GC14643

AZD8330 (ARRY-424704) は強力で非競合的な MEK1/MEK2 阻害剤であり、IC50 は 7 nM です。

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AZD8330 化学構造

Cas No.: 869357-68-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$88.00
在庫あり
5mg
$87.00
在庫あり
10mg
$160.00
在庫あり
50mg
$466.00
在庫あり
100mg
$654.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

MOS, U2OS, KPD, ZK58, 143b and Saos-2 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 ~ 1 μM; 72 hrs

Applications

AZD8330 decreased viability of MOS and U2OS cells, and significantly affected 143b cells. In contrast, AZD8330 exhibited no effect on viability of KPD, ZK58 and Saos-2 cells. According to a capase3/7 activity assay, AZD8330 at the concentration of 0.5μM induced apoptosis in MOS and U2OS cells, but not in KPD and ZK58 cells.

References:

[1]. Zuzanna Baranski, Tijmen H. Booij, Marieke L. Kuijjer, Yvonne de Jong, Anne-Marie Cleton-Jansen, Leo S. Price, Bob van de Water, Judith V. M. G. Bovée, Pancras C.W. Hogendoorn, Erik H.J. Danen. MEK inhibition induces apoptosis in osteosarcoma cells with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov; 6(11-12): 503–512.

Background

AZD8330 is an orally active and selective MEK1/2 inhibitor with an IC50 of 7 nM. The inhibition of MEK1/2 by this component results in inhibition of growth factor-mediated cell signaling and tumor cell proliferation.

MEK, also known as MAP kinase kinase (MAP2K), is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). The activation of MAPK signaling pathway was shown to be involved in regulation of various cell processes including cell proliferation, differentiation, apoptosis, metabolism and inflammation.

AZD8330 treatment was shown to cause cell apoptosis by suppressing the activation of ERK1/2 signal transduction pathway in Burkitt's lymphoma cell line Raji cells, which is in a dose and time dependent manner [1].

Recently, a large phase I trial of 82 patients with advanced tumor malignancies was conducted to define the maximum tolerated dose (MTD) and assessed the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8330. The MTD of this product was determined as 40mg/day [2].

References:
1.  Feng K, Wang C, Zhou H, Yang J, Dong L, Zhou K, et al. [Effect of ERK1/2 inhibitor AZD8330 on human Burkitt's lymphoma cell line Raji cells and its mechanism]. Zhonghua Xue Ye Xue Za Zhi 2015,36:148-152.
2.  Cohen RB, Aamdal S, Nyakas M, Cavallin M, Green D, Learoyd M, et al. A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies. Eur J Cancer 2013,49:1521-1529.

Chemical Properties

Cas No. 869357-68-6 SDF
同義語 ARRY-424704; ARRY-704; AZD-8330; ARRY424704; ARRY704; AZD8330
Chemical Name 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide
Canonical SMILES CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO
Formula C16H17FIN3O4 M.Wt 461.23
溶解度 ≥ 23.05mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1681 mL 10.8406 mL 21.6812 mL
5 mM 0.4336 mL 2.1681 mL 4.3362 mL
10 mM 0.2168 mL 1.0841 mL 2.1681 mL
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計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

レビュー

Review for AZD8330

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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