VER-50589

Catalog No.S7459

VER-50589 Chemical Structure

Molecular Weight(MW): 388.80

VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.

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Biological Activity

Description VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Targets
HSP90β [1]
21 nM
In vitro

VER-50589 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 143 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-50589 causes induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5, which further result in cell cycle arrest and apoptosis. [1]

In vivo In HCT116 human colon cancer xenografts, VER-50589 (100 mg/kg i.p.) results in a statistically significant reduction of ∼30% in tumor volume and weight, as well as induction of HSP72 and depletion of ERBB2 and C-RAF. [1]

Protocol

Kinase Assay:[1]
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Fluorescence Polarization Assay:

Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.
Cell Research:[1]
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  • Cell lines: Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: HCT116 human colon cancer xenografts
  • Formulation: 10% DMSO, 5% Tween 20, 85% saline
  • Dosages: ~100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.04 mM)
Ethanol 77 mg/mL (198.04 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.80
Formula

C19H17ClN2O5

CAS No. 747413-08-7
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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HSP (e.g. HSP90) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID