Home Apoptosis Bcl-2 inhibitor VU661013 For research use only.

VU661013

VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.

VU661013 Chemical Structure

VU661013 Chemical Structure

CAS No. 2131184-57-9

Purity & Quality Control

Batch: S875801 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.70%
98.70

VU661013 Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

Biological Activity

Description VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
Targets
MCL1 [1]
(Cell-free assay)
97 pM(Ki)
In vitro
In vitro

VU661013 is 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.[1]
Cell Research Cell lines MV4-11 cells
Concentrations 100 nM - 5 μM
Incubation Time 48 h
Method

To generate cells that are resistant to BCL-2 or MCL-1 inhibition, MV4-11 cells are treated over the course of 3 months with gradually increasing concentrations of VEN (5nM to 2.5 μM) or VU661013 (100nM 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.
In Vivo
In vivo

VU661013 is active in patient derived xenografts. In addition, VU661013 is safely combined with venetoclax for synergy in murine models of AML.[1]
Animal Research Animal Models 6–8 weeks old female NSGS [NOD-scid IL2Rgnull3Tg(hSCF/hGM-CSF/hIL3)] mice
Dosages 10 mg/kg, 25 mg/kg, 75 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 712.66 Formula

C39H39Cl2N5O4
CAS No. 2131184-57-9 SDF --
Smiles CC1CN(C(=O)C2=C(C3=C(N12)C(=C(C=C3)Cl)C4=C(N(N=C4C)C)C)CCCOC5=CC(=C(C(=C5)C)Cl)C)C6=CN(C7=C6C=C(C=C7)C(=O)O)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (140.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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