Bemcentinib-R428-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBemcentinibCat. No.: HY-15150CAS No.: 1037624-75-1Synonyms: R428; BGB324分式: CHN分量: 506.64作靶點: TAM Receptor作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 10.

2、25 mg/mL (20.23 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.9738 mL 9.8689 mL 19.7379 mL5 mM 0.3948 mL 1.9738 mL 3.9476 mL10 mM 0.1974 mL 0.9869 mL 1.9738 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Bemcentinib (R428)種效的具有選擇性的 Axl 抑制劑

3、，IC50 值為 14 nM。IC50 & Target IC50: 14 nM (Axl kinase)體外研究Bemcentinib (R428) (2M) significantly interferes with mechanisms of migration and invasion of Axlposmelanoma cells at levels comparable to Axl knockdown 1. Bemcentinib (R428) synergizes with CDDP to1/3 Master of Small Molecules 您邊的抑制劑師www.MedC

4、hemEenhance suppression of liver micrometastasis 2. Bemcentinib (R428) (50 nM-1M) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipiduptake 3.體內(nèi)研究 Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3

5、H2LN metastasesdevelopment in two independent mouse models of breast cancer dissemination, suppresses both tumorangiogenesis 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 h

6、igh-fat diet resulted insignificantly reduced weight gain and subcutaneous and gonadal fat mass 3.PROTOCOLCell Assay 1 Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber(1.5105 cells per well) of uncoated (migration) or matrigel-coated (invasion) 24

7、-well chambers. RPMImedium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 M) orvehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both theupper and lower chambers contain the drug or vehicle. Quantification of migrat

8、ing/invading cells is obtainedby measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20or 42 hours later, respectively.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Seven- to 8-wk-old female N

9、Cr nu/nu mice are injected intracardially with bioluminescent MDA-MB-231-luc-Administration 2 D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by in v

10、ivobioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cancer Cell. 2018 Dec 10;34(6):954-969.e4. Theranostics. 2018 Jul 30;8(15):4262-4278. J Cell Mol Med. 2019 Jun

11、 26. Sci Rep. 2017 Dec 19;7(1):17770. Faculty of Medicine. University of Oslo. 2019 Feb.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptorkinase. J Inve

12、st Dermatol. 2011 Dec;131(12):2448-57.2. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models ofmetastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue developmentin mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64.McePdfHeightC