1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

APS-2-79 

Cat. No.: HY-100627 Purity: 99.21%
Data Sheet SDS Handling Instructions

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $70 In-stock
25 mg $130 In-stock
50 mg $220 In-stock
100 mg $400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of APS-2-79:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

In Vitro

APS-2-79 inhibits BRAF and CRAF phosphorylation of MEK in a KSR-dependent manner. APS-2-79 does not affect BRAF(V600E)-induced MAPK activation in cells. APS-2-79 impedes KSR-stimulated MAPK signalling within cells through wild-type and MEK equally. APS-2-79 synergizes with trametinib specifically in Ras-mutant cells compared to the HER-family and SRC-family inhibitors lapatinib and sarcatinib. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. The IC50 value of APS-2-79 against ATPbiotin probe-labelling of KSR2 is 120 nM[1].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[1]

APS-2-79 is dissolved in DMSO.

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 timecourse of assays. Specifically, 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 for 72 hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors for 72 hrs. Cell viability is measured using resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

387.43

Formula

C₂₃H₂₁N₃O₃

CAS No.

2002381-25-9

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

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