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Brigatinib

Brigatinib
Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.
Catalog No. T3621Cas No. 1197953-54-0
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Purity:100%
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Brigatinib

Catalog No. T3621Cas No. 1197953-54-0
Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$43In Stock
10 mg$61In Stock
25 mg$88In Stock
50 mg$116In Stock
100 mg$169In Stock
200 mg$253In Stock
500 mg$428In Stock
1 mL x 10 mM (in DMSO)$59In Stock
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Product Introduction

Bioactivity
Description
Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.
Targets&IC50
IGF-1R:24.9 nM, ALK:0.37 nM, FLT3:2.1 nM, ROS1:1.9 nM, EGFR (C797S/del19):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].
Kinase Assay
In vitro HotSpotSM kinase profiling of 289 kinases is performed. The assay is conducted in the presence of 10 μM [33P]-ATP, using brigatinib concentrations ranging from 0.05 nM to 1 μM.
Cell Research
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)
AliasAP-26113
Chemical Properties
Molecular Weight584.09
FormulaC29H39ClN7O2P
Cas No.1197953-54-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 5.84 mg/mL (10 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7121 mL8.5603 mL17.1206 mL85.6032 mL
5 mM0.3424 mL1.7121 mL3.4241 mL17.1206 mL
10 mM0.1712 mL0.8560 mL1.7121 mL8.5603 mL

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