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Description: Bemcentinib (formerly known as BGB324; R428) is a novel, potent and selective inhibitor of the RTK (receptor tyrosine kinase) Axl with potential anticancer activity. It inhibits Axl with an IC50 of 14 nM, and shows > 100-fold higher selectivity for Axl over Abl. R428 showed high activity in blocking tumor spread and prolonging survival in animal models with metastatic breast cancer. Axl signaling regulates breast cancer metastasis at multiple levels in tumor cells and tumor stromal cells and that selective Axl blockade by R428 confers therapeutic value in prolonging survival of animals bearing metastatic tumors.
References: Cancer Res. 2010 Feb 15; 70(4):1544-54; Blood. 2011 Feb 10; 117(6):1928-37.
Related CAS: 1037624-91-1 (racemic); 1037624-75-1;
(S)-1-(6, 7-dihydro-5H-benzo[6, 7]cyclohepta[1, 2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6, 7, 8, 9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1, 2, 4-triazole-3, 5-diamine
Exact Mass: 506.29064
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