AP26113-analog (ALK-IN-1)

Catalog No.S7000 Batch:S700002

Technical Data

Formula

C₂₆H₃₄ClN₆O₂P

Molecular Weight

529.01

CAS No.

1197958-12-5

Solubility (25°C)*

In vitro

DMSO

106 mg/mL (200.37 mM)

Ethanol

106 mg/mL (200.37 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

NMP 1 PEG 300 (10 2 90, v 3 v)

10.0mg/ml

Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of 1 ml NMP+PEG 300 (10+90, v+v) clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)	View More
0.07 nM	28.4 nM	32 nM	36.8 nM	36.8 nM	View More

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 Assay:^{^[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.

Cell Assay:^{^[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.

References

Customer Product Validation

: , , Clin Cancer Res,2015, 21(1):166-74.

Selleck's AP26113-analog (ALK-IN-1) has been cited by 5 publications

Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion–Positive Cancer [Katayama R, et al. Clin Cancer Res, 2015, 21(1):166-74]	PubMed: 25351743
Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib [ Clin Cancer Res, 2014, 20(22):5686-96]	PubMed: 25228534
Two Novel ALK Mutations Mediate Acquired Resistance to the Next-Generation ALK Inhibitor Alectinib [Katayama R, et al. Clin Cancer Res, 2014, 20(22):5686-96]	PubMed: 25228534
A New Human Lung Adenocarcinoma Cell Line Harboring the EML4-ALK Fusion Gene [Isozaki H, et al. Jpn J Clin Oncol, 2014, 44(10):963-8]	PubMed: 25170107
Establishment and Characterization of a Singaporean Chinese Lung Adenocarcinoma Cell Line with Four Copies of the Epidermal Growth Factor Receptor Gene [Choong ML, et al. Biores Open Access, 2014, 3(4):176-82]

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.