Bemcentinib-d8

Bemcentinib-d8 (R428-d8) is the deuterium labeled Bemcentinib. Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].

Product Specifications

Product Name Alternative

R428-d8; BGB324-d8

UNSPSC

12352005

Target

Isotope-Labeled Compounds; TAM Receptor

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

NC1=NC(NC2=CC(CC[C@@H](N3C([2H])([2H])C([2H])([2H])C([2H])([2H])C3([2H])[2H])CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6

Molecular Formula

C30H26D8N8

Molecular Weight

514.69

References & Citations

[1]Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131 (12) :2448-57. |[2]Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70 (4) :1544-54.