Brigatinib

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC[1].

Product Specifications

CAS Number

[1197953-54-0]

Product Name Alternative

AP-26113

UNSPSC

12352005

Hazard Statement

H302, H317, H318, H335, H412

Target

Anaplastic lymphoma kinase (ALK)

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Brigatinib.html

Purity

99.98

Solubility

DMSO : 2 mg/mL (ultrasonic) |Ethanol : 10 mg/mL (ultrasonic; warming)

Smiles

CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1

Molecular Formula

C29H39ClN7O2P

Molecular Weight

584.09

Precautions

H302, H317, H318, H335, H412

References & Citations

[1]Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22 (22) :5527-5538|[2]Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59 (10) :4948-64.|[3]Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7 (20) :29011-22