APS-2-79 hydrochloride | 赛默飞Alfa aesar官网

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APS-2-79 hydrochloride

APS-2-79 hydrochloride 是一种 KSR 依赖性的 MEK 拮抗剂。APS-2-79 与 ATP^biotin 竞争性地结合到 KSR2-MEK1 复合物内的 KSR2，IC₅₀ 为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态，使其无法再结合 RAF 和激活 MEK，从而阻断了 Ras-MAPK 信号通路。

APS-2-79 hydrochloride Chemical Structure

CAS No. : 2002381-31-7

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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APS-2-79 hydrochloride 的其他形式现货产品:

APS-2-79

生物活性

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^[1].

IC₅₀ & Target^[1]

KSR2

120 nM (IC₅₀)

MEK1

体外研究
(In Vitro)

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]

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

423.89

Formula

C₂₃H₂₂ClN₃O₃

CAS 号

2002381-31-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

Cell Assay ^[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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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.

Cell Assay
^[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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