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VU0661013

SKU: orb1706470

Description

VU0661013 is a potent and selective MCL-1 inhibitor used in cancer research. It is employed in vitro to study apoptosis and has demonstrated antitumor activity in vivo models, aiding the investigation of BCL-2 family protein dynamics and therapeutic strategies.

Research Area

Cell Biology

Images & Validation

Key Properties

CAS Number2131184-57-9
MW712.66
Purity99.46% (May vary between batches)
FormulaC39H39Cl2N5O4
SMILESC[C@@H]1CN(c2cn(C)c3ccc(cc23)C(O)=O)C(=O)c2c(CCCOc3cc(C)c(Cl)c(C)c3)c3ccc(Cl)c(-c4c(C)nn(C)c4C)c3n12
TargetBcl-2 Family
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.61 mM);DMSO:117 mg/mL (164.17 mM)

Bioactivity

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) .
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 .

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Mcl-1, VU661013, VU-661013, VU0661013, VU-0661013, VU 661013, VU 0661013
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Protocol Information

VU0661013 (orb1706470)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,430.00
5 mg
¥ 2,730.00
1 ml x 10 mM (in DMSO)
¥ 2,860.00
10 mg
¥ 3,640.00
25 mg
¥ 5,590.00
50 mg
¥ 7,280.00
DispatchUsually dispatched within 3-5 working days
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