Brigatinib-d11

Brigatinib-d11 (AP-26113-d11) is deuterium labeled 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

[2055306-76-6]

Product Name Alternative

AP-26113-d11

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK) ; Isotope-Labeled Compounds

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

COC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)P(C)(C)=O)=N2)C=CC(N4CCC(N5C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C5([2H])[2H])C([2H])([2H])[2H])CC4)=C1

Molecular Formula

C29H28D11ClN7O2P

Molecular Weight

595.16

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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]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|[4]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