Bemcentinib (GMP)  (Synonyms: R428 (GMP); BGB324 (GMP))

Bemcentinib (R428) GMP is an orally active and selective inhibitor of Axl with an IC₅₀ of 14 nM^[1][2].

IC50: 14 nM (Axl kinase)^[1][2].

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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

506.64

C₃₀H₃₄N₈

1037624-75-1

NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131(12):2448-57.  [Content Brief]

  [2]. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54.  [Content Brief]

  [3]. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64.  [Content Brief]