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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Cited by 5 Publications

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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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
NCT03737994 Not yet recruiting ALK Gene Rearrangement|ALK Positive|Lung Non-Squamous Non-Small Cell Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 National Cancer Institute (NCI) April 1 2019 Phase 2
NCT03737994 Not yet recruiting ALK Gene Rearrangement|ALK Positive|Lung Non-Squamous Non-Small Cell Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 National Cancer Institute (NCI) April 1 2019 Phase 2
NCT03868423 Not yet recruiting Advanced Malignant Neoplasm|ALK Fusion Protein Expression|ALK Gene Amplification|ALK Gene Mutation|Locally Advanced Malignant Solid Neoplasm|Metastatic Malignant Neoplasm in the Brain|Metastatic Malignant Neoplasm in the Central Nervous System|Metastatic Malignant Solid Neoplasm|ROS1 Fusion Positive|ROS1 Gene Amplification|ROS1 Gene Mutation Sameek Roychowdhury|National Cancer Institute (NCI)|Ohio State University Comprehensive Cancer Center March 31 2019 Phase 2
NCT03420742 Not yet recruiting Carcinoma Advanced ALK+ or ROS1+Non-Small-Cell Lung Neoplasm Advanced ALK+ or ROS1+Solid Tumors Ariad Pharmaceuticals|Takeda March 28 2019 Phase 1
NCT03868423 Not yet recruiting Advanced Malignant Neoplasm|ALK Fusion Protein Expression|ALK Gene Amplification|ALK Gene Mutation|Locally Advanced Malignant Solid Neoplasm|Metastatic Malignant Neoplasm in the Brain|Metastatic Malignant Neoplasm in the Central Nervous System|Metastatic Malignant Solid Neoplasm|ROS1 Fusion Positive|ROS1 Gene Amplification|ROS1 Gene Mutation Sameek Roychowdhury|National Cancer Institute (NCI)|Ohio State University Comprehensive Cancer Center March 31 2019 Phase 2
NCT03420742 Not yet recruiting Carcinoma Advanced ALK+ or ROS1+Non-Small-Cell Lung Neoplasm Advanced ALK+ or ROS1+Solid Tumors Ariad Pharmaceuticals|Takeda March 28 2019 Phase 1

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID