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ChemicalBook--->CAS DataBase List--->1668553-26-1

1668553-26-1

1668553-26-1 Structure

1668553-26-1 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07,GHS09
[Signal word ]

Warning
[Hazard statements ]

H302-H400-H410
[Precautionary statements ]

P264-P270-P273-P301+P312-P330-P391-P501
Hazard InformationBack 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.
Spectrum DetailBack Directory
[Spectrum Detail]

A-1210477(1668553-26-1)1HNMR
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