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]. |