Brigatinib (AP26113) - 2mM in DMSO, high purity , CAS No.1197953-54-0

Item Number

B420874

• Synonyms: Brigatinib | 1197953-54-0 | ALUNBRIG | AP-26113 | Brigatinib [USAN] | UNII-HYW8DB273J | HYW8DB273J | Brigatinib (AP-26113) | AP 26113 | (2-((5-chloro-2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide |
• Specifications & Purity: Moligand™, 2mM in DMSO
• Biochemical and Physiological Mechanisms: Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Brigatinib (AP26113) Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

Targets

ALK (Cell-free assay); ROS1 (Cell-free assay); FLT3 (Cell-free assay); IGF1R (Cell-free assay); EGFR(C797S/del19) (cell-based) 16489,0.37 nM; 1.9 nM ;2.1 nM; 24.9 nM; 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. 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_max=448 ng/mL,t_1/2=5.8 h. And in CD rats, after dosing at 3 mg/kg i.v, CL=0.46 L/(h·kg), t_1/2=4.8 h, Vss=7.8 L/kg; Dosed at 10 mg/kg p.o, Cmax=305 ng/mL, t_max=4 h, t_1/2=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.

Cell Research(from reference)

Cell lines：U937 cells, Karpas-299 cells, H3122 cells 

Incubation Time：72 h