Brigatinib

• Product Name Alternative:

  AP-26113

• UNSPSC Description:

  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].

• Target Antigen:

  Anaplastic lymphoma kinase (ALK)

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• 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 Weight:

  584.09

• 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

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Launched

• CAS Number:

  1197953-54-0