1. Apoptosis
  2. Bcl-2 Family
  3. VU0661013


Cat. No.: HY-112859 Purity: 98.42%
Handling Instructions

VU661013 is a potent and selective MCL-1 inhibitor.

For research use only. We do not sell to patients.

VU0661013 Chemical Structure

VU0661013 Chemical Structure

CAS No. : 2131184-57-9

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 862 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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VU661013 is a potent and selective MCL-1 inhibitor.

IC50 & Target[1]



In Vitro

VU661013 exhibits 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. However, VU661013 does not significantly inhibit BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM)[1].

In Vivo

VU661013, a novel, potent, selective MCL-1 inhibitor that de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in Venetoclax-resistant cells and patient derived xenografts. After establishing disseminated leukemia, NSGS mice are dosed intraperitoneally with 10, 25 or 75 mg/kg of VU661013 daily for 21 days. Weekly chimerism analyses are conducted and the percentage of MV-4-11 cells are quantified in murine peripheral blood using anti-human CD45 (hCD45) and anti-hCD33 monoclonal antibodies. Twenty-eight days post-transplant, vehicle-treated mice have developed large leukemia burdens and thus, mice are sacrificed, and their organs are harvested for analysis. Vehicle mice treated died of xenografted AML, but have no evidence of VU661013-related toxicity in non target organs. VU661013 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 VU661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amendeding spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In a second MV-4-11 xenograft study, mice are followed until death, and survival is evaluated by Kaplan-Meier analysis. In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU661013. 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].

Molecular Weight







ClC1=CC=C(C(CCCOC2=CC(C)=C(Cl)C(C)=C2)=C3N4[[email protected]](C)CN(C5=CN(C)C6=C5C=C(C(O)=O)C=C6)C3=O)C4=C1C7=C(C)N(C)N=C7C


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (175.40 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4032 mL 7.0160 mL 14.0319 mL
5 mM 0.2806 mL 1.4032 mL 2.8064 mL
10 mM 0.1403 mL 0.7016 mL 1.4032 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.92 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution

*All of the co-solvents are provided by MCE.
Cell Assay

To generate cells that are resistant to BCL-2 or MCL-1 inhibition, MV-4-11 cells are treated over the course of 3 months with gradually increasing concentrations of VEN (5 nM to 2.5 μM) or VU661013 (100 nM to 5 μM). Cells are declared to be VEN or VU661013-resistant when they are able to maintain 100% viability in the presence of these high concentrations (5 μM of VU661013 and 2.5 μM of VEN) of inhibitors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Upon establishing microchimerism, mice are treated with either Venetoclax by daily gavage, VU661013 (10, 25 or 75 mg/kg) by daily i.p injection, or vehicle. VU661013 is dissolved in DMSO and diluted in ethanol, Polyethylene Glycol (PEG), and saline. Venetoclax is dissolved in PEG and ethanol, and diluted with Phosal 50 PG. Peripheral blood is assessed weekly for human chimerism. Spleen/body ratio is calculated as organ weight (gram) per gram of body weight[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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VU0661013VU 0661013VU-0661013Bcl-2 FamilyInhibitorinhibitorinhibit

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