APS-2-79 hydrochloride

Name: APS-2-79 hydrochloride
Brand: MedChemExpress
SKU: HY-100627A
Rating: 5.0 (1 reviews)

Cat. No.: HY-100627A Purity: 98.42%: Data Sheet
COA

SDS
Handling Instructions
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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.

For research use only. We do not sell to patients.

APS-2-79 hydrochloride Chemical Structure

CAS No. : 2002381-31-7

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of APS-2-79 hydrochloride:

APS-2-79 In-stock

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•Related Screening Libraries:

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View All MEK Isoform Specific Products:

View All Isoforms

MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

KSR2

120 nM (IC₅₀)

MEK1

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]

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

Molecular Weight

423.89

Formula

C₂₃H₂₂ClN₃O₃

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.42%

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Data Sheet (280 KB) SDS (761 KB)

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

Handling Instructions (2659 KB)

References

[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]

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].

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

References

[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