Home Protein Tyrosine Kinase ALK inhibitor - EGFR inhibitor AP26113-analog (ALK-IN-1) For research use only.

AP26113-analog (ALK-IN-1)

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

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

CAS: 1197958-12-5

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

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Purity & Quality Control

Batch: Purity: 99.94%
99.94

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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
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 529.01 Formula

C26H34ClN6O2P
CAS No. 1197958-12-5 SDF Download AP26113-analog (ALK-IN-1) SDF
Smiles CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 106 mg/mL ( (200.37 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 106 mg/mL

Water : Insoluble


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In vivo
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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.
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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

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