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

Key Properties

• CAS Number: 2131184-57-9
• MW: 712.66
• Purity: 99.46% (May vary between batches)
• Formula: C₃₉H₃₉Cl₂N₅O₄
• SMILES: C[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
• Target: Bcl-2 Family
• Solubility: 10% 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) .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

134828256