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Brigatinib

Catalog No. T3621   CAS 1197953-54-0
Synonyms: AP-26113

Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.

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Brigatinib Chemical Structure
Brigatinib, CAS 1197953-54-0
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 61.00
25 mg In stock $ 93.00
50 mg In stock $ 116.00
100 mg In stock $ 169.00
200 mg In stock $ 253.00
500 mg In stock $ 428.00
1 mL * 10 mM (in DMSO) In stock $ 59.00
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Purity: 100%
Purity: 99.93%
Purity: 99.51%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.
Targets&IC50 FLT3:2.1 nM, ROS1:1.9 nM, ALK:0.37 nM, IGF1R:24.9 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)
Synonyms AP-26113
Molecular Weight 584.09
Formula C29H39ClN7O2P
CAS No. 1197953-54-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 5.84 mg/mL (10 mM)

TargetMolReferences and Literature

1. Wei-Sheng Huang, et al. J Med Chem, 2016, 59(10):4948-4964. 2. Uchibori, K et al. Nat. Commun. 8, 14768 doi: 10.1038/ncomms14768 (2017).

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Keywords

Brigatinib 1197953-54-0 Angiogenesis Immunology/Inflammation JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR FLT ROS IGF-1R ALK Inhibitor inhibit ALK tyrosine kinase receptor AP26113 CD246 AP 26113 Anaplastic lymphoma kinase (ALK) AP-26113 Cluster of differentiation 246 Anaplastic lymphoma kinase inhibitor

 

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