1197953-54-0

Product Details:

CasNo： 1197953-54-0

Molecular Formula： C29H39ClN7O2P

Purity： 99%

Synonyms: AP26113 (Brigatinib); Brigatinib, AP26113; 5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine; 5-chloro-N4-(2-(dimethylphosphoryl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine; brigatib; 140455; Bogtinib (AP26113)
Melting point: >203°C
Boiling point: 781.8±70.0 °C
Density: 1.31±0.1 g/cm3
Solubility: Soluble in DMSO (1 mg/ml with warming)
Color: White to off-white
Form: solid
Pka: 8.14±0.42
Storage temp.: Store at -20°C

General Description：
Brigatinib (AP26113) is a medicine used to treat cancer that suppresses epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK). Brigatinib is a selective agonist against variations of EGFR as opposed to the wild mutant forms. The drug also illustrates selectivity against the ALK-EML4 fusion gene, which is a fundamental aspect of the modification of susceptible lung parenchyma. Brigatinib is prescribed for patients with specific abnormal genes and when the non-small cell lung cancer (NSCLC) is non-responsive to management with other medications. Brigatinib is classified as a kinase inhibitor, whose mechanism of action entails suppressing the action of abnormal proteins that enhance the multiplication of cancer cells.
 

Indications：
Brigatinib is prescribed for patients with specific forms of NSCLC that have spread to various sections of the body in people who have been on previous treatment with other cancer medications such as crizotinib, and their condition has become worse or they indicate minimal signs of improvement.
 

Pharmacodynamics：
Brigatinib suppresses in vitro viability and proliferation of cells which indicate the EML4-ALK protein fusion and 17 crizotinib-resistant ALK variations. The drug action spreads to cells illustrating EGFR deletions, FLT3-D835Y, FLT3-F691L and ROS1-L2026M. Brigatinib encapsulates a dose-dependent obstruction of tumor burden, tumor growth and prolonged survival.
 

Mechanism of Action：
Brigatinib is a tyrosine kinase suppressor with activity against specific kinases such as ROS1, ALK, point mutations, EGFR deletions, and insulin-like development factor 1 receptor. The drug acts by suppressing the operation of downstream indicating proteins and ALK phosphorylation.