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Home > Products >  Bemcentinib (R428)

Bemcentinib (R428) CAS NO.1037624-75-1

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Keywords

  • Bemcentinib (R428)
  • BGB324
  • 1037624-75-1

Quick Details

  • ProName: Bemcentinib (R428)
  • CasNo: 1037624-75-1
  • Molecular Formula: C30H34N8
  • ProductionCapacity: Metric Ton/Day
  • Purity: >97%
  • LimitNum: 0 Metric Ton

Superiority

Biological Activity

Description Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
Targets
Axl [1]
(Cell-free assay)
14 nM
In vitro

R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. [1] In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM 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 μM) under similar experimental conditions. [2]
Cell Data
 
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells Function assay   1 h   Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA, IC50=0.03 μM 26555154
H1299 Growth inhibiton assay   48 h   R428 inhibited growth of H1299 in a dose-dependent manner with an IC50 of approximately 4 μM. 30210917
LM3 cells Function assay 2.5 μM 0-36 h   R428 induced cytoplasmic vacuoles within one hour after R428 treatment, and the vacuoles increased in number and size with time. 30210917

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot   30210917
Growth inhibition assay 30210917
Immunofluorescence   30210917 26670048
In vivo Pharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. [1]

 

 

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