Home Angiogenesis ALK inhibitor - FLT3 inhibitor - EGFR inhibitor - ROS1 inhibitor - IGF-1R inhibitor Brigatinib For research use only.

Brigatinib

Synonyms: AP26113

Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

Brigatinib Chemical Structure

Brigatinib Chemical Structure

CAS: 1197953-54-0

Selleck's Brigatinib has been cited by 33 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay, GI50 = 0.01 μM. 27144831
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50 = 0.029 μM. 27144831
Ba/F3 Function assay 72 hrs Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay, GI50 = 0.0672 μM. 29136465
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50 = 0.26 μM. 30429956
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50 = 0.42 μM. 30429956
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50 = 1.09 μM. 30429956
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50 = 3.194 μM. 27144831
KARPAS299 Antitumor assay 50 mg/kg 13 days Antitumor activity against human KARPAS299 cells expressing NMP-ALK fusion protein xenografted in SCID/beige mouse assessed as tumor regression at 50 mg/kg, po administered once daily for 13 days, NULL = NULL μM. 27144831
Click to View More Cell Line Experimental Data

Biological Activity

Description Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, 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)		 Click to View More Targets
0.37 nM 1.9 nM 2.1 nM 24.9 nM 39.9 nM
In vitro
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].
Cell Research 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).
Experimental Result Images Methods Biomarkers Images PMID
Western blot pEGFR / EGFR / pAkt / Akt / pERK / ERK / pS6 / S6 pALK / ALK pROS1 / ROS1 / pSTAT3 / STAT3 28287083
Growth inhibition assay Cell viability 25351743
In Vivo
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].
Animal Research Animal Models female CD rats
Dosages 10 mg/kg(p.o); 2 mg/kg(i.v)
Administration p.o, i.v
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06132867 Not yet recruiting Healthy Volunteers Takeda December 18 2023 Phase 1
NCT04925609 Recruiting Anaplastic Large Cell Lymphoma ALK-Positive|Inflammatory Myofibroblastic Tumor|Other Solid Tumor Princess Maxima Center for Pediatric Oncology|Takeda August 18 2022 Phase 1|Phase 2
NCT04718012 Completed Lung Cancer ROS Translocated Centre Hospitalier Intercommunal Creteil March 17 2021 --
NCT04634110 Terminated Brain Metastases|Lung Cancer University of Colorado Denver|National Cancer Institute (NCI) November 17 2020 Phase 2
NCT04260009 Withdrawn Anaplastic Lymphoma Kinase Positive (ALK +) Anaplastic Large Cell Lymphoma|Inflammatory Myofibroblastic Tumors|Solid Tumors Takeda September 1 2020 Phase 1|Phase 2
NCT04111705 Active not recruiting Non Small Cell Lung Cancer Metastatic Intergroupe Francophone de Cancerologie Thoracique August 5 2020 Phase 2

Chemical lnformation & Solubility

Molecular Weight 584.09 Formula

C29H39ClN7O2P
CAS No. 1197953-54-0 SDF --
Smiles CN1CCN(CC1)C2CCN(CC2)C3=CC(=C(C=C3)NC4=NC=C(C(=N4)NC5=CC=CC=C5P(=O)(C)C)Cl)OC
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 43 mg/mL

DMSO : 1 mg/mL ( (1.71 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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