A 1210477

Key Product Details

Product Description

A 1210477 is a selective, high affinity Mcl-1 inhibitor (K_i = 454 pM). Disrupts Mcl-BIM complexes (IC₅₀ in low μM range). Also inhibits Mcl-1NOXA interactions. Exhibits no effect on Bcl-X_L-Bim or Bcl-X-BCL-X_s interactions. Induces apoptosis in multiple myeloma and non-small cell lung cancer cell lines and exhibits a synergistic effect with Navitoclax^TM to induce apoptosis in vitro. Cell permeable.

Product Specifications for A 1210477

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

Solubility

Preparing Stock Solutions for A 1210477

The following data is based on the product molecular weight 850.04.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.02 mM	58.82 mL	294.10 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

Calculators

Background References

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

• Leverson 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. 2015 PMID: 25590800
• Bruncko Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity. J.Med.Chem. 2015 PMID: 25679114

Product Documents for A 1210477