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Bemcentinib (R428)
| Product Name | Bemcentinib (R428) |
| Price: | Inquiry |
| Catalog No.: | CN00490 |
| CAS No.: | 1037624-75-1 |
| Molecular Formula: | C30H34N8 |
| Molecular Weight: | 506.64 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | N=c1nc([nH]n1c1nnc2c(c1)CCCc1c2cccc1)Nc1ccc2c(c1)CC[C@H](CC2)N1CCCC1 |
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| Description | Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM. |
| Target | IC50: 14 nM (Axl kinase) |
| In Vitro | Bemcentinib (R428) (2μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown[1]. Bemcentinib (R428) synergizes with cisplatin to enhance suppression of liver micrometastasis[2]. Bemcentinib (R428) (50 nM-1μM) 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]. |
| Cell Assay | Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber (1.5×105 cells per well) of uncoated (migration) or matrigel-coated (invasion) 24-well chambers. RPMI medium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 μM) or vehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both the upper and lower chambers contain the drug or vehicle. Quantification of migrating/invading cells is obtained by measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20 or 42 hours later, respectively. |
| Animal Admin | Seven- to 8-wk-old female NCr nu/nu mice are injected intracardially with bioluminescent MDA-MB-231-luc-D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins 2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by in vivo bioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 799.6±70.0 °C at 760 mmHg |
| Flash Point | 437.4±35.7 °C |
| Exact Mass | 506.290649 |
| PSA | 98.51000 |
| LogP | 4.55 |
| Vapour Pressure | 0.0±2.8 mmHg at 25°C |
| Storage condition | -20℃ |