A-1155463 Hydrochloride

CAS: 1235034-55-5

Ref. TR-A100800

Product Information

• Name: A-1155463 Hydrochloride
• Synonyms: 2-[8-[(2-Benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]-4-thiazolecarboxylic Acid Hydrochloride
• CAS: 1235034-55-5

Description

Applications A-1155463 Hydrochloride, is a potent and selective BCL-XL inhibitor with in vivo activity. A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of <0.01nM (<10 pM), highly selective against closely related proteins of BCL-2 (Ki = 74nM, >7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 , represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2-BIM, complexes, killi
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Zhang, H., et al.: Mol. Cancer, 14, 1 (2015); Tao, Z., et al.: ACS Med. Chem. Lett., 5, 1088 (2014)

• Brand: TRC

Chemical properties

• Molecular weight: 706.25
• Formula: C₃₅H₃₂FN₅O₄S₂•HCl
• Color/Form: Beige Solid
• InChI: InChI=1S/C35H32FN5O4S2.ClH/c1-40(2)17-6-8-22-14-15-28(26(36)20-22)45-19-7-13-30-31(33(43)44)38-35(47-30)41-18-16-23-9-5-10-24(25(23)21-41)32(42)39-34-37-27-11-3-4-12-29(27)46-34;/h3-5,9-12,14-15,20H,7,13,16-19,21H2,1-2H3,(H,43,44)(H,37,39,42);1H
• SMILES: CN(C)CC#Cc1ccc(OCCCc2sc(N3CCc4cccc(C(=O)Nc5nc6ccccc6s5)c4C3)nc2C(=O)O)c(F)c1.Cl