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
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Brigatinib
Dangerous GoodsCAS number：1197953-54-0 molecular formula：C29H39ClN7O2P
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 1197953-54-0 | NCGC00483924-01 | (2-((5-chloro-2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide | 2,4-Pyrimidinediamine, 5-chloro-N4-(2-(dimethylphosphinyl)phenyl)-N2-(2-methoxy-4-( | ||
| CAS number | 1197953-54-0 | molecular formula | C29H39ClN7O2P |
| molecular weight | 584.09 g/mol | Exact mass | - |
| PSA | 85.900 Ų | logp | 5.084 |
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Safety information
pictogram：
GHS06 , GHS08 , GHS09
Signal word：
Danger
Hazard Statement：
H301: 吞咽会中毒 H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子
Statement of Preventive Measures：
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 P318: 如果暴
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