High Purity in bulk supply1037624-75-1 R428 in stock CAS NO.1037624-75-1

 Bemcentinib, also known as BGB-324 or R428, is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.

R428 is a small molecule inhibitor of Axl kinase, both in an in vitro biochemical assay and in a cell-based assay using phosphorylation of Ser⁴⁷³ on Akt as the readout (EC₅₀s = 14 nM for both). It is orally bioavailable, blocks angiogenesis in corneal micropocket and tumor models, and reduces metastatic burden while extending survival in mouse models of breast cancer metastasis. R428 synergizes with cisplatin to enhance suppression of liver micrometastasis. R428 is used to study the role of Axl kinase signaling in cancer, cellular senescence, and Zika virus infection.

Potent and selective inhibitor of AXL kinase (IC₅₀ = 14 nM). Overcomes chemotherapy resistance to various agents in multiple cancer models. Suppresses myeloid cell activation and function.  AXL inhibition combined with PD-1 blockade shows potent synergistic anti-tumor effects. Greater than 100-fold selective for AXL versus ABL. Selective (50-100-fold) versus Mer and Tyro3 in cell-based assays. Highly selective for AXL versus InsR, EGFR, HER2, and PDGFRbeta in cell-free assays.