Overview

  • Product name

    A-1210477, MCL-1 inhibitor
  • Description

    Potent, selective MCL-1 inhibitor
  • Biological description

    Potent, selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members. Cell permeable. Binds to MCL-1 selectively and with sufficient affinity to disrupt the MCL-1-BIM complex in living cells, achieving the hallmarks of intrinsic apoptosis, and demonstrating clear-on-target cancer cell killing capability either as a single agent or in combination with ABT-263 (Navitoclax).

  • Purity

    > 99%
  • CAS Number

    1668553-26-1
  • Chemical structure

    Chemical Structure

Properties

  • 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
  • Molecular weight

    850.04
  • Molecular formula

    C46H55N7O7S
  • PubChem identifier

    66575373
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 3 mM (with warming)
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC1=NN(C(=C1C2=CC=CC3=C2N(C(=C3CCCOC4=CC=CC5=CC=CC=C54)C(=O)O)CCN6CCOCC6)COC7=CC=C(C=C7)N8CCN(CC8)S(=O)(=O)N(C)C)C
  • Source

    Synthetic

References

This product has been referenced in:

  • Leverson JD  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 Dis 6:e1590 (2015). Read more (PubMed: 25590800) »
  • Xiao Y  et al. MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor. Mol Cancer Ther 14:1837-47 (2015). Read more (PubMed: 26013319) »
  • Phillips DC  et al. Loss in MCL-1 function sensitizes non-Hodgkin's lymphoma cell lines to the BCL-2-selective inhibitor venetoclax (ABT-199). Blood Cancer J 5:e368 (2015). Read more (PubMed: 26565405) »

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