Overview

  • Product name

    R428 (BGB324), AXL inhibitor
  • Description

    Potent and selective AXL kinase inhibitor
  • Biological description

    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.  

  • Purity

    > 98%
  • General notes

    Solutions in DMSO may be stored at -20°C for up to 3 months.

  • CAS Number

    1037624-75-1
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    1-(3,4-Diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine

  • Molecular weight

    506.64
  • Molecular formula

    C30H34N8
  • PubChem identifier

    46215462
  • Storage instructions

    Shipped at Room Temperature. Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 25 mM

  • Handling

    Toxic, refer to SDS for further information.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    c1ccc-2c(c1)CCCc3c2nnc(c3)n4c(nc(n4)Nc5ccc6c(c5)CC[C@H](CC6)N7CCCC7)N
  • Source

    Synthetic

References

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) »

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