Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
1.7121 mL
8.5603 mL
17.1206 mL
5 mM
0.3424 mL
1.7121 mL
3.4241 mL
10 mM
0.1712 mL
0.8560 mL
1.7121 mL
50 mM
0.0342 mL
0.1712 mL
0.3424 mL
Description
Brigatinib (AP26113) is a potent and selective (IC50, 0.6 nM) and (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
Targets
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. 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): C=448 ng/mL,t=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, t=4 h, t=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.
