A 1210477

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Cat.No. 6409 - A 1210477 | C46H55N7O7S | CAS No. 1668553-26-1
Description: Selective, high affinity Mcl-1 inhibitor; proapoptotic
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

Selective, high affinity Mcl-1 inhibitor (Ki = 454 pM). Disrupts Mcl-BIM complexes (IC50 in low μM range). Also inhibits Mcl-1NOXA interactions. Exhibits no effect on Bcl-XL-Bim or Bcl-X-BCL-Xs interactions. Induces apoptosis in multiple myeloma and non-small cell lung cancer cell lines and exhibits a synergistic effect with NavitoclaxTM to induce apoptosis in vitro. Cell permeable.

Technical Data

M. Wt 850.04
Formula C46H55N7O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1668553-26-1
PubChem ID 66575373
InChI Key XMVAWGSQPHFXKU-UHFFFAOYSA-N
Smiles CN(C)S(=O)(=O)N1CCN(CC1)C1=CC=C(OCC2=C(C(C)=NN2C)C2=C3N(CCN4CCOCC4)C(C(O)=O)=C(CCCOC4=CC=CC5=C4C=CC=C5)C3=CC=C2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 1.7 2 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 850.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.02 mM 58.82 mL 294.1 mL 588.21 mL
0.1 mM 11.76 mL 58.82 mL 117.64 mL
0.2 mM 5.88 mL 29.41 mL 58.82 mL
1 mM 1.18 mL 5.88 mL 11.76 mL

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References

References are publications that support the biological activity of the product.

Bruncko et al (2015) Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity. J.Med.Chem. 58 2180 PMID: 25679114

Leverson et al (2015) 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 Dis. 6 e1590 PMID: 25590800


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Citations for A 1210477

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Literature in this Area

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Cancer

Cancer Research Product Guide

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  • Epigenetics in Cancer
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  • Invasion and Metastasis
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Parkinson's

Parkinson's Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.

Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for A 1210477

Apoptosis

Apoptosis Signaling Pathway

Apoptosis is a physiological process for cell death that is critical during aging and development. It may also be referred to as cell 'suicide'. Apoptosis can be triggered by events both inside and outside of the cell.