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Submit ReviewA 1210477
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)
Biological Activity for A 1210477
A 1210477 is a 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 for A 1210477
| 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.
Product Datasheets for A 1210477
References for A 1210477
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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Keywords: A 1210477, A 1210477 supplier, A1210477, Mcl-1, inhibitors, inhibits, apoptosis, proapoptotic, selective, high, affinity, multiple, myeloma, non-small, cell, lung, cancer, Bcl-2, Family, 6409, Tocris Bioscience
Citations for A 1210477
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Parkinson's Disease 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 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
