AP26113-analog (ALK-IN-1)

Catalog No.S7000

For research use only.

AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.

AP26113-analog (ALK-IN-1) Chemical Structure

CAS No. 1197958-12-5

Selleck's AP26113-analog (ALK-IN-1) has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
Targets
ALK [1]
(Cell-free assay)
EGFR(C797S/del19) [2]
(Cell-free assay)
IGF1R [1]
(Cell-free assay)
EGFR(del19) [1]
(Cell-free assay)
EGFR(del19) [2]
(Cell-free assay)
Click to View More Targets
0.07 nM 28.4 nM 32 nM 36.8 nM 36.8 nM
In vitro

Brigatinib and AP26113-analog have similar potency against the triple-mutant EGFR with IC50 values of <100 nM. AP26113-analog suppresses phosphorylation of EGFR and its downstream signalling pathway in cells expressing all types of EGFR mutations[2].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Ba/F3 cells
  • Concentrations: 0.3 nM to 10 μM
  • Incubation Time: 72 h
  • Method:

    Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3 nM to 10 μM. After 72 h of drug treatment, cell viability is measured using the CellTiter-Glo assay.

Solubility (25°C)

In vitro

Ethanol 106 mg/mL
(200.37 mM)
DMSO 45 mg/mL
(85.06 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
NMP+PEG300 (10+90, v+v)
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 529.01
Formula

C26H34ClN6O2P

CAS No. 1197958-12-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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