A-1155463 Hydrochloride

Catalogue number: A100800
Chemical 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;
Impurity:
CAS Number: NA
Possible CAS #: NA
Molecular form.: C₃₅H₃₂FN₅O₄S₂•HCl
Appearance: Beige Solid
Melting Point: >140°C (dec.)
Mol. Weight: 669.793646
Storage: -20°C Freezer, Under inert atmosphere
Solubility: Chloroform (Slightly, Heated), DMSO (Slightly)
Stability: No Data Available
Category: No Data Available
Boiling Point: No Data Available
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, kil
Dangerous Goods Info: NA
References:
Peer Review Product Citations: Kotapati, S. et al.: Chem. Res. Toxicol. (2011) 24: 1516-26 PMID: 21749114
Kumaran Sivagnanam et al. J Sci Food Agr (2017) DOI: 10.1002/jsfa.7703
Ádám Tölgyesi et al. J Food Add Cont (2015) PMID: 26212568
Park JE et al. Xenobiotica. 2008 Sep;38(9):1240-51 PMID: 18720283
Lee HB. et al. Chemosphere. 2009 Nov;77(10):1285-91 PMID: 19863993
Bapiro TE. Anal Chem. 2016 Jun 21;88(12):6190-4 PMID: 27228284
1) Aizawa K. et. al, 2016. Int J Cancer. 1;139(5):1171-81. PMID: 27116542
2) Narayanapillai SC, et. al, 2016. Chem Res Toxicol. PMID: 27728767
3) Moghbel N. et. al, 2016. Toxicol Lett. 8;254:45-51 PMID: 27178269
4) Narauanapillai SC, et al, 2016. Drug Metab Dispos. 44(3):422-7. PMID: 26744252
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