| Identification | Back Directory | [Name]
A-1210477 | [CAS]
1668553-26-1 | [Synonyms]
CS-2202
CS-2151
A-1210477
Abbvie Mcl-1 Inhibitor
A-1210477;A 1210477;A1210477
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
7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid
1H-Indole-2-carboxylic acid, 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]- | [Molecular Formula]
C46H55N7O7S | [MDL Number]
MFCD28399118 | [MOL File]
1668553-26-1.mol | [Molecular Weight]
850.04 |
| Chemical Properties | Back Directory | [Boiling point ]
1027.4±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
insoluble in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
Powder | [pka]
4.43±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
A-1210477 is an inhibitor of the antiapoptotic Bcl-2 family protein myeloid cell leukemia-1 (Mcl-1; Ki = 0.43 nM and IC50 = 26.2 nM) that demonstrates >100-fold selectivity over other Bcl-2 family members (Kis > 0.66 μM for Bcl-2, Bcl-XL, Bcl-W, and Bfl-1). It has been shown to disrupt the interaction between Mcl-1 and pro-apoptotic BIM, inducing the hallmarks of apoptosis in Mcl-1-dependent multiple myeloma and non-small cell lung cancer cell lines. | [Uses]
Abbvie Mcl-1 Inhibitor is an inhibitor of Mcl-1 where Mcl-1 is an anti-apoptotic. | [References]
[1]. lopez j, bessou m, riley js, et al. mito-priming as a method to engineer bcl-2 addiction. nature communications, 2016, 7:10538.
[2]. besbes s, mirshahi m, pocard m, et al. new dimension in therapeutic targeting of bcl-2 family proteins. oncotarget, 2015, 6(15): 12862.
[3]. leverson jd, zhang h, chen j, et al. potent and selective small-molecule mcl-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with abt-263 (navitoclax). cell death & disease, 2015, 6(1): e1590.
[4]. mott jl, kobayashi s, bronk sf, et al. mir-29 regulates mcl-1 protein expression and apoptosis. oncogene, 2007, 26(42): 6133-6140.
[5]. opferman jt. attacking cancer's achilles heel: antagonism of anti-apoptotic bcl-2 family members. febs journal, 2015. |
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