Product nameR428 (BGB324), AXL inhibitor
DescriptionPotent and selective AXL kinase inhibitor
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.
Solutions in DMSO may be stored at -20°C for up to 3 months.
Storage instructionsShipped at Room Temperature. Store at -20°C. Store under desiccating conditions.
Soluble in DMSO to 25 mM
Toxic, refer to SDS for further information.
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This product has been referenced in:
- Ludwig KF et al. Small-Molecule Inhibition of Axl Targets Tumor Immune Suppression and Enhances Chemotherapy in Pancreatic Cancer. Cancer Res 78:246-255 (2018). Read more (PubMed: 29180468) »
- Ben-Batalla I et al. Axl Blockade by BGB324 Inhibits BCR-ABL Tyrosine Kinase Inhibitor-Sensitive and -Resistant Chronic Myeloid Leukemia. Clin Cancer Res 23:2289-2300 (2017). Read more (PubMed: 27856601) »
- Lin JZ et al. Targeting AXL overcomes resistance to docetaxel therapy in advanced prostate cancer. Oncotarget 8:41064-41077 (2017). Read more (PubMed: 28455956) »
- Guo Z et al. Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models. Oncotarget 8:89761-89774 (2017). Read more (PubMed: 29163786) »
- Meertens L et al. Axl Mediates ZIKA Virus Entry in Human Glial Cells and Modulates Innate Immune Responses. Cell Rep 18:324-333 (2017). Read more (PubMed: 28076778) »
- Brand TM et al. AXL Is a Logical Molecular Target in Head and Neck Squamous Cell Carcinoma. Clin Cancer Res 21:2601-12 (2015). Read more (PubMed: 25767293) »
- Jin CW et al. Gas6 delays senescence in vascular smooth muscle cells through the PI3K/ Akt/FoxO signaling pathway. Cell Physiol Biochem 35:1151-66 (2015). Read more (PubMed: 25766527) »
- Fleuren ED et al. The role of AXL and the in vitro activity of the receptor tyrosine kinase inhibitor BGB324 in Ewing sarcoma. Oncotarget 5:12753-68 (2014). Read more (PubMed: 25528764) »
- Ghosh AK et al. The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy. Blood 117:1928-37 (2011). Read more (PubMed: 21135257) »
- 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 70:1544-54 (2010). Read more (PubMed: 20145120) »