VER-49009

Catalog No.S7458 Synonyms: CCT0129397

VER-49009 Chemical Structure

Molecular Weight(MW): 387.82

VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.

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Biological Activity

Description VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
Targets
HSP90β [1]
47 nM
In vitro

VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. [1] VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis. [2]

In vivo In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2. [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: Mice bearing established OVCAR3 human ovarian xenografts.
  • Formulation: 10% DMSO, 5% Tween 20, 85% saline
  • Dosages: ~4 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.54 mM)
Water Insoluble
Ethanol 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 387.82
Formula

C19H18ClN3O4

CAS No. 940289-57-6
Storage powder
in solvent
Synonyms CCT0129397

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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