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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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.
Purity & Quality Control
Choose Selective ALK Inhibitors
|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.|
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. Brigatinib overcomes the resistance of EGFR-triple-mutant and the activity depends on ATP-competitive manner with less affection to wild-type EGFR.
|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. 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.|
|In vitro||Ethanol||43 mg/mL warmed (73.61 mM)|
|DMSO||1 mg/mL warmed (1.71 mM)|
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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||--|
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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