1668553-26-1

Basic information

• Product Name: A-1210477
• Synonyms: A-1210477;Abbvie Mcl-1 Inhibitor;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;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
• CAS NO: 1668553-26-1
• Molecular Formula: C46H55N7O7S
• Molecular Weight: 850.0366
• Product Categories: Inhibitors
• Mol File: 1668553-26-1.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 1027.4±65.0 °C(Predicted)
• Appearance: /
• 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
• PKA: 4.43±0.30(Predicted)
• CAS DataBase Reference: A-1210477(CAS DataBase Reference)
• NIST Chemistry Reference: A-1210477(1668553-26-1)
• EPA Substance Registry System: A-1210477(1668553-26-1)

Safety Data

• Hazardous Substances Data: 1668553-26-1(Hazardous Substances Data)

Usage

Description

A-1210477 is an inhibitor of the antiapoptotic Bcl-2 family protein myeloid cell leukemia-1 (Mcl-1), which plays a crucial role in preventing programmed cell death. With a Ki value of 0.43 nM and an IC50 value of 26.2 nM, A-1210477 exhibits over 100-fold selectivity for Mcl-1 compared to other Bcl-2 family members. A-1210477 has been demonstrated to disrupt the interaction between Mcl-1 and pro-apoptotic BIM, leading to the induction of apoptosis in Mcl-1-dependent multiple myeloma and non-small cell lung cancer cell lines.

Uses

Used in Oncology:
A-1210477 is used as an anticancer agent for targeting Mcl-1, an anti-apoptotic protein that is overexpressed in various cancers. By inhibiting Mcl-1, A-1210477 promotes apoptosis in cancer cells, particularly in multiple myeloma and non-small cell lung cancer cell lines. This selective inhibition of Mcl-1 can potentially enhance the effectiveness of cancer treatments and improve patient outcomes.
Used in Drug Development:
A-1210477 is used as a lead compound in the development of novel therapeutics for cancer treatment. Its high selectivity for Mcl-1 makes it a valuable starting point for designing new drugs that can target this protein with minimal off-target effects. This could lead to the development of more effective and safer cancer treatments.
Used in Research:
A-1210477 is used as a research tool for studying the role of Mcl-1 in apoptosis and cancer cell survival. Its ability to selectively inhibit Mcl-1 makes it a valuable compound for investigating the molecular mechanisms underlying cell death and the development of resistance to cancer therapies. This can help researchers better understand the biology of cancer and identify new targets for therapeutic intervention.

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.