All AbMole products are for research use only, cannot be used for human consumption.
Bemcentinib (R428) blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. Bemcentinib (R428) inhibited angiogenesis in corneal micropocket and tumor models.
In vitro, Bemcentinib (R428) caused a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake.
In vivo, oral administration of Bemcentinib (R428) for 5 weeks to mice kept on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass. Additionally, Bemcentinib (R428) synergized with cisplatin to enhance suppression of liver micrometastasis.
Cancer Biol Ther. 2015 Oct;1535-47.
The small GTPase ADP-Ribosylation Factor 1 mediates the sensitivity of triple negative breast cancer cells to EGFR tyrosine kinase inhibitors.
Bemcentinib purchased from AbMole
Cell Experiment | |
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Cell lines | MDA-MB-231 or 4T1 cells |
Preparation method | Invasion Assays: MDA-MB-231 or 4T1 cells (1 × 105) were allowed to migrate through Matrigel (Millipore) toward 20% FCS in an 8-μm pore 24-well Transwell plate (BD Bio‐sciences) at 37°C for 16 to 24 h. Noninvaded cells and Matrigel were removed by swabbing. Invaded cells were fixed in 4% formaldehyde, stained with 1% crystal violet, and quantified as for Axl cellbased assay. Cells were preincubated with R428 for 3 h. R428 was added to both upper and lower Transwell chambers. |
Concentrations | 0, 0.03, 0.3, 3 µ M |
Incubation time | 3 h |
Animal Experiment | |
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Animal models | Female BALB/c mice 4T1 Orthotopic Model |
Formulation | R428 was formulated for in vivo studies in 0.5% hydroxypropylmethylcellulose + 0.1% Tween 80. |
Dosages | 7–75 mg/kg twice daily |
Administration | oral gavage |
Molecular Weight | 506.64 |
Formula | C30H34N8 |
CAS Number | 1037624-75-1 |
Solubility (25°C) | DMSO 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Products are for research use only. Not for human use. We do not sell to patients.
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