AP26113-analog (ALK-IN-1)

Catalog No.S7000 Batch:S700001

Print

Technical Data

Formula

C26H34ClN6O2P
Molecular Weight 529.01 CAS No. 1197958-12-5
Solubility (25°C)* In vitro Ethanol 106 mg/mL (200.37 mM)
DMSO 45 mg/mL (85.06 mM)
Water Insoluble
* <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
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.

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
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.