VER-50589

Catalog No.S7459 Batch:S745901

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Technical Data

Formula

C19H17ClN2O5
Molecular Weight 388.80 CAS No. 747413-08-7
Solubility (25°C)* In vitro DMSO 77 mg/mL (198.04 mM)
Ethanol 77 mg/mL (198.04 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • 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.
Animal Study:[1]
  • Animal Models

    HCT116 human colon cancer xenografts

  • Dosages

    ~100 mg/kg

  • Administration

    i.p.

Selleck's VER-50589 has been cited by 3 publications

Antiviral activity of the HSP90 inhibitor VER-50589 against enterovirus 71 [ Antiviral Res, 2023, 211:105553] PubMed: 36737007
Evolution of kinase polypharmacology across HSP90 drug discovery [ Cell Chem Biol, 2021, S2451-9456(21)00221-X] PubMed: 34077750
A Repurposing Strategy for Hsp90 Inhibitors Demonstrates Their Potency against Filarial Nematodes [Gillan V, et al. PLoS Negl Trop Dis, 2014, 8(2):e2699] PubMed: 24551261

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.