CH5138303

Catalog No.S7340 Batch:S734001

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Technical Data

Formula

C19 H18 Cl N5 O2 S
Molecular Weight 415.9 CAS No. 959763-06-5
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.56 mM)
Water Insoluble
Ethanol 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 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
Targets
HSP90α [1]
(Cell-free assay)
0.48 nM(Kd)
In vitro CH5138303 shows high affinity to Hsp90αand potent cell growth inhibitory activity against an HCT116 colorectal cancer cell line and an NCI-N87 gastric cancer cell line with IC50 of 98 nM and 66 nM, respectively. [1] Besides, CH5138303 also demonstrates liver microsomal stability. [1]
In vivo CH5138303 (50 mg/kg p.o.) displays high oral bioavailability in mice and produces potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.[1]

Protocol (from reference)

Kinase Assay:

[1]
  • Surface plasmon resonance direct binding assay for Hsp90α

    Measurements are performed on a Biacore2000 at a flow rate of 30 μL/min, 25 °C in 50 mM Tris-based saline, pH 7.6, 0.005% Tween20 and 1% DMSO. Biotinylated N-terminal Hsp90α (9–236) is coupled on a streptavidin-coated surface of a sensorchip to a density of ca. 2000 RU.
Cell Assay:

[1]
  • Cell lines

    HCT116 and NCI-N87 cell lines

  • Concentrations

    ~10 μM

  • Incubation Time

    4 days

  • Method

    HCT116 cell line and NCI-N87 cell line are cultured according to the supplier’s instructions. Cells suspended in a medium are added to solutions containing various concentrations of the test substance, and the cells are cultured at 37 °C in 5% CO2. Four days later, Cell Counting Kit-8 solution is added and absorbance at 450 nm is measured with Microplate-Reader iMark. Antiproliferative activity is calculated by the formula (1−T/C) × 100 (%), where T represents the absorbance of drug-treated cells and C that of untreated control cells at 450 nm. The 50% inhibition concentration (IC50) values are calculated using Microsoft Excel 2007.
Animal Study:

[1]
  • Animal Models

    Mice with human NCI-N87 gastric cancer xenograft.

  • Dosages

    50 mg/kg

  • Administration

    p.o.

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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.