R428 [1037624-75-1]

Catalog number: HY-15150_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: 5 mg
10 mM
10 mg
50 mg
Price: € 552.60 € 614.00
Expected delivery time: 10 days

Product specifications for - R428 [1037624-75-1]

Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 1037624-75-1
Purity: >98%
Molecular Formula: C30H34N8
Molecular weight: 506.6446
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: R428 is a potent and selective small-molecule inhibitor (IC50=14 nM), blocks the activities of Axl. IC50 value: 14 nM [1] Target: Axl kinase in vitro: R428 exhibited potent activity (EC50/IC50, 14 nM) in both in vitro biochemical kinase assays using recombinant Axl protein and a cell-based assay reflecting Axl signaling in HeLa cells that uses downstream phosphorylation of Akt on Ser473 as the readout. R428 potently blocked autophosphorylation on a COOH-terminal multiple docking site, Tyr821, stimulated by either antibody-mediated cross-linking or Gas6[1]. Pharmacological inhibition of Axl with R428 in EAC cell lines significantly reduced anchorage-independent growth, invasion and migration [2]. in vivo: Pharmacologic investigations revealed favorable exposure after oral administration such that R428-treated tumors displayed a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail [1]. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of 2 uM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 uM) under similar experimental conditions. R428 inhibits angiogenesis in corneal micropocket and tumor models.
Safety information: 
Additional information: 
Synonyms: HY-15150; R-428; R 428; BGB324; BGB-324; BGB 324
Targeting AXL overcomes resistance to docetaxel therapy in advanced prostate cancer', Lin JZ. Oncotarget. 2017 Jun 20;8(25):41064-41077. Read more
Cell softening in malignant progression of human lung cancer cells by activation of receptor tyrosine kinase AXL', Iida K. Sci Rep. 2017 Dec 19;7(1):17770. Read more