AP26113-analog (ALK-IN-1)

Catalog No.S7000

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

Molecular Weight(MW): 529.01

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.

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1 Customer Review

  • Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins.

    Clin Cancer Res,2015, 21(1):166-74.. AP26113-analog (ALK-IN-1) purchased from Selleck.

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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)
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

Cell Research:

[2]

+ Expand
  • 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.


    (Only for Reference)

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 individually and in order:
NMP+polyethylene glycol 300 (10+90, v+v)
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 529.01
Formula

C26H34ClN6O2P

CAS No. 1197958-12-5
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02094573 Active, not recruiting Non-small Cell Lung Cancer|Lung Cancer|Advanced Malignancies|Carcinoma Ariad Pharmaceuticals March 2014 Phase 2
NCT01449461 Unknown status Advanced Malignancies|Carcinoma, Non-Small-Cell Lung|Anaplastic Large Cell Lymphoma|Diffuse Large Cell Lymphoma|Inflammatory Myofibroblastic Tumors Ariad Pharmaceuticals September 2011 Phase 1|Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID