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Medchemexpress LLC 1H-Indole-5-carboxylic acid, 3-[(4R)-7-chloro-10-[3-(4-chloro-3,5-dimethylphenoxy)propyl]-3,4-dihy | 2131184-57-9 | 98.5% | 712.66 | 25 MG
SDP

Supplier:  Medchemexpress LLC 25MGHY112859

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VU661013 is a potent and selective MCL-1 inhibitor. It exhibits a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK. However, VU661013 does not significantly inhibit BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM).

  • VU661013 is a novel, potent, selective MCL-1 inhibitor that de-stabilizes BIM/MCL-1 association.
  • It leads to apoptosis in AML.
  • It is active in Venetoclax-resistant cells and patient derived xenografts.
  • Treatment with VU661013 results in a dose-dependent decrease in tumor burden in disseminated human AML.

Catalog No. 50-004-39263


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