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
Biological ActivityA 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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Bruncko 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).
Leverson et al.
Cell Death Dis., 2015;6:e1590
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