1. MAPK/ERK Pathway
  2. MEK
  3. APS-2-79

APS-2-79 

Cat. No.: HY-100627 Purity: 99.31%
Handling Instructions

APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin 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 Chemical Structure

APS-2-79 Chemical Structure

CAS No. : 2002381-25-9

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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
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10 mg USD 70 In-stock
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25 mg USD 140 In-stock
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50 mg USD 230 In-stock
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100 mg USD 400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin 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

 

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]

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

Molecular Weight

387.43

Formula

C₂₃H₂₁N₃O₃

CAS No.
SMILES

CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=NC=NC4=CC(OC)=C(OC)C=C43

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 : 20 mg/mL (51.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (5.16 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (5.16 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.16 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
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Keywords:

APS-2-79MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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Product Name:
APS-2-79
Cat. No.:
HY-100627
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