Brigatinib (AP26113)

Catalog No.S8229

Brigatinib (AP26113) Chemical Structure

Molecular Weight(MW): 584.09

Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

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1 Customer Review

  • Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.

    Mol Cancer Res, 2017, 15(1):106-114. Brigatinib (AP26113) purchased from Selleck.

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Choose Selective ALK Inhibitors

Biological Activity

Description Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
Targets
ALK [1]
(Cell-free assay)		 ROS1 [1]
(Cell-free assay)		 FLT3 [1]
(Cell-free assay)		 IGF1R [1]
(Cell-free assay)		 EGFR(C797S/del19) [2]
(cell-based)
0.37 nM 1.9 nM 2.1 nM 24.9 nM 39.9 nM
In vitro

Beyond ALK, IGF1R, and InsR, brigatinib also potently inhibits FLT3 and ROS1 with IC50 values of 2.1 and 1.9 nM, respectively. It does not show significant activity toward c-Met or Ron up to 1 μM[1]. Brigatinib overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR[2].
In vivo Mouse PK parameters for Brigatinib following oral dosing (10 mg/kg): Cmax=448 ng/mL,t1/2=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t1/2=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, tmax=4 h, t1/2=3.4 h， F%=52. Brigatinib demonstrates dose-dependent antitumor activity[1]. Brigatinib demonstrates growth inhibition activity in PC9 triple-mutant xenograft model and in combination with anti-EGFR antibody to potentiate the efficacy both in vitro and in vivo as shown in first-generation EGFR-TKI-resistant patients[2].

Protocol

Cell Research:

[1]
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  • Cell lines: U937 cells, Karpas-299 cells, H3122 cells
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    All cell lines were used within 20 passages of the initial thaw. Following inhibitor treatment for 72 h, cell growth was assessed to determine the concentration that causes 50% inhibition of cell viability (IC50).


    (Only for Reference)
Animal Research:

[1]
+ Expand
  • Animal Models: female CD rats
  • Formulation: --
  • Dosages: 10 mg/kg(p.o); 2 mg/kg(i.v)
  • Administration: p.o, i.v
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 43 mg/mL warmed (73.61 mM)
DMSO 1 mg/mL warmed (1.71 mM)
Water 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.

Chemical Information

Molecular Weight 584.09
Formula

C29H39ClN7O2P
CAS No. 1197953-54-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02706626 Recruiting Non-Small Cell Lung Cancer Criterium Inc.|University of Colorado Denver|Duke University|Takeda|Vanderbilt University|University of Texas Southwestern Medical Center March 9 2017 Phase 2
NCT02094573 Active not recruiting Carcinoma Non-Small-Cell Lung Ariad Pharmaceuticals June 4 2014 Phase 2
NCT03707938 Not yet recruiting Advanced Lung Carcinoma|ALK Gene Rearrangement|Non-Small Cell Lung Carcinoma|Recurrent Non-Small Cell Lung Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 M.D. Anderson Cancer Center|National Cancer Institute (NCI) March 31 2019 Early Phase 1
NCT03420742 Not yet recruiting Carcinoma Advanced ALK+ or ROS1+Non-Small-Cell Lung Neoplasm Advanced ALK+ or ROS1+Solid Tumors Ariad Pharmaceuticals|Takeda October 29 2018 Phase 1
NCT02737501 Active not recruiting Non-small Cell Lung Cancer|Lung Cancer|Advanced Malignancies|Carcinoma Ariad Pharmaceuticals|Takeda May 26 2016 Phase 3
NCT03389399 Recruiting Non-Small Cell Lung Cancer Academic Thoracic Oncology Medical Investigators Consortium|Takeda Pharmaceuticals International Inc.|University of Colorado Denver February 22 2018 --

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.

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID