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VU0661013

Catalog No. T17247 CAS 2131184-57-9

Synonyms: VU661013

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

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VU0661013, CAS 2131184-57-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 179.00
5 mg	In stock	$ 455.00
10 mg	In stock	$ 672.00
25 mg	In stock	$ 1,060.00
50 mg	In stock	$ 1,430.00
100 mg	In stock	$ 1,920.00
1 mL * 10 mM (in DMSO)	In stock	$ 490.00

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Purity: 99.46%

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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].

Synonyms	VU661013
Molecular Weight	712.66
Formula	C39H39Cl2N5O4
CAS No.	2131184-57-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 117mg/mL (164.2mM)

References and Literature

1. Haley E. Ramsey, et al. A Novel MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia. Cancer Discov. August 28, 2018.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max PPI Inhibitor Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

VU0661013 2131184-57-9 Apoptosis BCL VU 661013 VU 0661013 VU661013 VU-661013 VU-0661013 inhibitor inhibit

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