Home Protein Tyrosine Kinase ALK inhibitor - EGFR inhibitor AP26113-analog (ALK-IN-1)

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AP26113-analog (ALK-IN-1) ALK inhibitor

Cat.No.S7000

AP26113-analog (ALK-IN-1) is a potent and selective ALK inhibitor, as well as an inhibitor of EGFR, and is an analog of AP26113.
AP26113-analog (ALK-IN-1) ALK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 529.01

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Chemical Information, Storage & Stability

Molecular Weight 529.01 Formula

C26H34ClN6O2P

 Storage (From the date of receipt)
CAS No. 1197958-12-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC

Solubility

In vitro
Batch:

DMSO : 106 mg/mL (200.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 106 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

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%DMSO %

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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.

Mechanism of Action

Targets/IC50/Ki
ALK [1]
(Cell-free assay)
0.07 nM
EGFR(C797S/del19) [2]
(Cell-free assay)
28.4 nM
IGF1R [1]
(Cell-free assay)
32 nM
EGFR(del19) [1]
(Cell-free assay)
36.8 nM
EGFR(del19) [2]
(Cell-free assay)
36.8 nM
EGFR(C797S/T790M/del19) [2]
(Cell-free assay)
59.1 nM
INSR [1]
(Cell-free assay)
100 nM
EGFR(T790M/del19) [2]
(Cell-free assay)
138.6 nM
In vitro
Brigatinib and AP26113-analog (ALK-IN-1) have similar potency against the triple-mutant EGFR with IC50 values of <100 nM. It suppresses phosphorylation of EGFR and its downstream signalling pathway in cells expressing all types of EGFR mutations[2].
References

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