An Mcl-1 inhibitor (Ki = 0.19 nM); induces cell death in multiple myeloma

S63845 – 5 mg

Brand:
Cayman
CAS:
1799633-27-4
Storage:
-20
UN-No:
Non-Hazardous - /

S63845 is an inhibitor of myeloid cell leukemia 1 (Mcl-1; Ki = 0.19 nM), a pro-survival protein that is overexpressed in many cancers.{32698} It induces cell death in multiple myeloma, leukemia, and lymphoma cell lines (IC50s = via mitochondrial apoptosis. S63845 acts synergistically with trametinib (Item No. 16292), lapatinib (Item No. 11493), PLX4032 (Item No. 10618), and erlotinib (Item No. 10483) to reduce proliferation of SK-MEL-2, BT474, A2058, and PC9 cells, respectively. S63845 (6.25-25 mg/kg) reduces tumor volume in an MV4-11 acute myeloid leukemia mouse xenograft model in a dose-dependent manner.  

 

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Description

An Mcl-1 inhibitor (Ki = 0.19 nM); induces cell death in multiple myeloma, leukemia, and lymphoma cell lines (IC50s = via mitochondrial apoptosis; acts synergistically with trametinib, lapatinib, PLX4032, and erlotinib to reduce proliferation of SK-MEL-2, BT474, A2058, and PC9 cells, respectively; reduces tumor volume in a MV4-11 acute myeloid leukemia mouse xenograft model in a dose-dependent manner

Formal name: α(R)-[[(5S)-5-[3-chloro-2-methyl-4-[2-(4-methyl-1-piperazinyl)ethoxy]phenyl]-6-(5-fluoro-2-furanyl)thieno[2,3-d]pyrimidin-4-yl]oxy]-2-[[1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl]methoxy]-benzenepropanoic acid

Synonyms: 

Molecular weight: 829.3

CAS: 1799633-27-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death|Apoptosis

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