Brigatinib

SKU: orb1303989

Description

Brigatinib (AP-26113) is a potent and selective small-molecule inhibitor of anaplastic lymphoma kinase (ALK). It is widely used in preclinical research, demonstrating efficacy in both in vitro cellular assays and in vivo models of ALK-positive cancers, particularly non-small cell lung carcinoma (NSCLC).

Research Area

Cardiovascular Research, Immunology & Inflammation, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1197953-54-0
• MW: 584.1
• Purity: >98%
• Formula: C₂₉H₃₉ClN₇O₂P
• SMILES: COc1cc(ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1)N1CCC(CC1)N1CCN(C)CC1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 1 mg/ml, warm)

Bioactivity

• Target IC50:
  IGF-1R:24.9 nM|ALK:0.37 nM|FLT3:2.1 nM|ROS1:1.9 nM|EGFR (C797S/del19):39.9 nM
• 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. 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.
• 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.
• 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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AP26113

Compound Identifiers

PubChem CID

68165256