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Bemcentinib(R428,BGB324)

  Cat. No.:  DC7258   Featured
Chemical Structure
1037624-75-1
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More than 5000 active chemicals with high quality for research!
Field of application
R428 is a potent and selective small-molecule inhibitor(IC50=14 nM), blocks the activities of Axl.
Cas No.: 1037624-75-1
Chemical Name: 1H-1,2,4-Triazole-3,5-diamine,1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-
Synonyms: R-428; R 428,BGB-324,BGB 324
SMILES: C1CCN(C1)[C@H]2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76
Formula: C30H34N8
M.Wt: 506.64
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
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].
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].
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