Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 5.84 mg/mL (10 mM)
You can also refer to dose conversion for different animals. More
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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