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Abbvie Mcl-1 Inhibitor

Synonyms: CT-A121;7-(5-((4-(4-(N,N-Dimethylsulfamoyl)piperazin-1-yl)phenoxy)methyl)-1,3-dimethyl-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic Acid;A-1210477
Cat. No.: A98150 CAS No.: 1668553-26-1
MDL.: Formula: C46H55N7O7S
F.W.850.04 Purity: 99%
Storage: Store at 0°C (short term), -20°C (long term)
 
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Catalog Number: A98150   CAS No.: 1668553-26-1
MDL: Formula: C46H55N7O7S
F.W.: 850.04 Purity: 99%
Package: Unit: mg
Appearance: M.P.:
B.P.: Density:
Optical Rotation: Refractive Index:
Solubility: Soluble in DMSO Stability:
Storage: Store at 0°C (short term), -20°C (long term) Category: Reference Standard
Reference: Zhong, Q., et. al.: Cell, 121, 1085 (2005); Opferman, J.T., et. al.: Science, 307, 1101 (2005);JD Leverson, et al, Potent and selective small-molecule MCL-1inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263(navitoclax), Cell Death & Disease (2015) 6, e1590; doi: 10.1038/cddis.2014.561
Application: Abbvie Mcl-1 Inhibitor is an inhibitor of Mcl-1 where Mcl-1 is an anti-apoptotic.A-1210477 is a proteolytically stable, cell-permeable and high affinity BH3 mimetics of anti-apoptotic protein MCL-1, binding to the target potently and selectively with a Ki value of 0.45 nM, highly selective against closely related proteins of BCL-2 (Ki = 132 nM, >290-fold selectivity) and BCL-XL (Ki > 660 nM, >1400-fold selectivity). A-1210477 is the first-in-class small molecule MCL-1 inhibitor with sufficient potency to disrupt the tight-binding MCL-1-BIM complex in living cells, achieving the hallmarks of intrinsic apoptosis, and demonstrating clear-on-target cancer cell killing capability either as a single agent or in combination with ABT-263 (Navitoclax).
Category: Aromatics, Inhibitors, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds