bgb-324

Bemcentinib (R428) belongs to small molecule inhibitors and is a highly selective oral Axl inhibitor (IC50 = 14 nM) with oral bioavailability and potent cell permeability. This compound effectively inhibits cancer cell migration and invasion, blocks tumor dissemination, and prolongs survival in various tumor models.

Bemcentinib-d8 (R428-d8) is the deuterium-labeled form of Bemcentinib. Bemcentinib (R428) is an orally active, selective Axl inhibitor with an IC50 of 14 nM. It inhibits cancer cell migration and invasion. In cells, its selectivity for Axl is over 100-fold greater than for Abl, and over 50- and 100-fold greater for the TAM family kinases Mer and Tyro3, respectively. Bemcentinib can prevent tumor spread in metastatic breast cancer models and extends survival.

(R)-Bemcentinib ((R)-R428) is the R-enantiomer of Bemcentinib. Known as a selective, orally active Axl inhibitor, Bemcentinib (R428) has an IC50 value of 14 nM. This compound can impede tumor spread and improve survival in models of metastatic breast cancer.

Brimarafenib is a selective RAF dimerization inhibitor, which can inhibit the activity of BRAF and CRAF, and exhibits significant inhibitory effects on a variety of RAF mutations (including BRAF I/II/III mutations, BRAF fusion and CRAF heterodimerization), and is used for the treatment of colorectal and pancreatic cancers and other solid tumors with MAPK mutations.