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VU0661013

Catalog No. T17247Cas No. 2131184-57-9
Alias VU661013

VU0661013 is an effective and selective inhibitor of MCL-1.

VU0661013

VU0661013

Purity: 99.46%
Catalog No. T17247Alias VU661013Cas No. 2131184-57-9
VU0661013 is an effective and selective inhibitor of MCL-1.
Pack SizePriceAvailabilityQuantity
1 mg$107In Stock
5 mg$273In Stock
10 mg$395In Stock
25 mg$636In Stock
50 mg$858In Stock
100 mg$1,150In Stock
1 mL x 10 mM (in DMSO)$294In Stock
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Purity:99.46%
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Product Introduction

Bioactivity
Description
VU0661013 is an effective and selective inhibitor of MCL-1.
In vitro
VU0661013 does not obviously suppress BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM). VU0661013 shows 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 [1].
In vivo
VU0661013 is a potent and selective MCL-1 inhibitor and is active in Venetoclax-resistant cells and patient-derived xenografts. VU0661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU0661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amending spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU0661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days) [1].
AliasVU661013
Chemical Properties
Molecular Weight712.66
FormulaC39H39Cl2N5O4
Cas No.2131184-57-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 117 mg/mL (164.2 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.4032 mL7.0160 mL14.0319 mL70.1597 mL
5 mM0.2806 mL1.4032 mL2.8064 mL14.0319 mL
10 mM0.1403 mL0.7016 mL1.4032 mL7.0160 mL
20 mM0.0702 mL0.3508 mL0.7016 mL3.5080 mL
50 mM0.0281 mL0.1403 mL0.2806 mL1.4032 mL
100 mM0.0140 mL0.0702 mL0.1403 mL0.7016 mL

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