Network Version
Bemcentinib Data Sheet
| Product Name: | Bemcentinib |
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| CAS No.: | 1037624-75-1 | |
| Cat. No.: | HY-15150 | |
| MWt: | 506.64 | |
| Formula: | C30H34N8 | |
| Purity : | >98% | |
| Solubility: | DMSO : 12.5 mg/mL (ultrasonic;warming;heat to 60°C) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].
IC50 & Target:IC50: 14 nM (Axl kinase)[1][2].
In Vitro:Bemcentinib (R428) (2 μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown[1]. Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis[2]. Bemcentinib (R428) (50 nM-1 μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake[3]. In Vivo:Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3H2LN metastases development in two independent mouse models of breast cancer dissemination, suppresses both tumor angiogenesis and vascular endothelial growth factor (VEGF)-induced corneal neovascularization in vivo[2]. Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) makes mice keep on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass[3]. |
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