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2 protocols using napabucasin

1

Drug Formulation and Preparation Protocol

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Napabucasin, panobinostat, and quisinostat were purchased from Selleckchem and A1331852 and Navitoclax from Chemietek, diluted in DMSO to make stock solutions, aliquoted and stored at −80C. Napabucasin was formulated by heating to 50C for 10 minutes and then sequentially adding 45% PEG300 (Sigma), 5% Tween80 (Sigma) and 45% sterile water, with vortexing after adding each component (Selleckchem). panobinostat was formulated by sequentially adding 48% PEG300 (Sigma), 2% Tween80 (Sigma) and 48% sterile water, with vortexing after adding each component (Selleckchem). quisinostat was formulated in 10% hydroxypropyl-b-cyclodextrin (Sigma), 25 mg/ml mannitol (Sigma), in sterile water(45 (link)). A1331852 was formulated by sequentially adding 10% Ethanol (Fisher), 60% Phosal 50 PG (Lipoid), and 30% PEG400 (Sigma), and vortexing (MedChemExpress). Navitoclax was formulated in 10% ethanol (Fisher), 30% PEG400 (Sigma), and 60% Phosal 50 PG (Lipoid), with vortexing after adding each component (MedChemExpress). Sorafenib was formulated in 90% corn oil (Selleckchem) with vortexing (MedChemExpress). Working solutions were made fresh prior to administration.
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2

Synthesis and Characterization of L61H46

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Napabucasin (BBI608) was purchased from Sigma-Aldrich Co. (St Louis, MO, USA). Erlotinib was purchased from Selleck Chemicals (Houston, TX, USA). L61H46 (Figure 1A), a MAC, was synthesized in our laboratory. The synthesis procedure was the same as our previous reports.25 (link) The compound L61H46 was recrystallized from CH2Cl2/CH3CH2OH, with a purity of 98.85% as determined by high performance liquid chromatography.
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