APS-2-79 hydrochloride

Name: APS-2-79 hydrochloride
Brand: MedChemExpress
SKU: HY-100627A
Rating: 5.0 (0 reviews)

製品番号: HY-100627A 純度: 98.42%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP^biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC₅₀ of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling.

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APS-2-79 hydrochloride 構造式

CAS 番号 : 2002381-31-7

容量	価格（税別）	在庫状況	数量
5 mg	$50	在庫あり	Estimated Time of Arrival: December 31
10 mg	$70	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of APS-2-79 hydrochloride:

APS-2-79 在庫あり

MEK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

KSR2

120 nM (IC₅₀)

MEK1

体外実験

APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells^[1].
APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

423.89

分子式

C₂₃H₂₂ClN₃O₃

CAS 番号

2002381-31-7

Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=C4C=C(OC)C(OC)=CC4=NC=N3.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (58.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3591 mL	11.7955 mL	23.5910 mL
5 mM	0.4718 mL	2.3591 mL	4.7182 mL
10 mM	0.2359 mL	1.1796 mL	2.3591 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 98.42%

Select Batch:

データシート (280 KB) SDS (761 KB)

COA (259 KB) HNMR (407 KB) LCMS (328 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116. [Content Brief]

細胞実験
^[1]

Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the time course of assays. A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs. Cell viability is measured using Resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls^[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3591 mL	11.7955 mL	23.5910 mL	58.9776 mL
	5 mM	0.4718 mL	2.3591 mL	4.7182 mL	11.7955 mL
	10 mM	0.2359 mL	1.1796 mL	2.3591 mL	5.8978 mL
	15 mM	0.1573 mL	0.7864 mL	1.5727 mL	3.9318 mL
	20 mM	0.1180 mL	0.5898 mL	1.1796 mL	2.9489 mL
	25 mM	0.0944 mL	0.4718 mL	0.9436 mL	2.3591 mL
	30 mM	0.0786 mL	0.3932 mL	0.7864 mL	1.9659 mL
	40 mM	0.0590 mL	0.2949 mL	0.5898 mL	1.4744 mL
	50 mM	0.0472 mL	0.2359 mL	0.4718 mL	1.1796 mL