CH5138303

Catalog No.S7340

CH5138303 Chemical Structure

Molecular Weight(MW): 415.9

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-N87 cells MnfDR5l1d3SxeHnjbZR6KGG|c3H5 MUW0JIRigXN? MnXDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNU56NzDj[YxteyCjZoTldkA1KGSjeYOgZpkhS0OtLUigZZN{[XluIFnDOVA:OC5yNk[g{txO M1nrblI1OzZ7OEO5
HCT116 cells NHv4OIdEgXSxdH;4bYNqfHliYYPzZZk> MlW1OEBl[Xm| M3XJfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1KGSjeYOgZpkhS0OtLUigZZN{[XluIFnDOVA:OC5yOUig{txO NFfoS5QzPDN4OUizPS=>
NCI-N87 cells NGT6dmtHfW6ldHnvckBie3OjeR?= M2\6XVAvODRidH:gOUB2VQ>? MX2yOEBp NUW5fY1xUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCQQ1mtUlg4KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDFS2ZTKHC{b4TlbY4hdGW4ZXygZZQhOC5yNDD0c{A2KHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{ NWH6SFdSOjR|Nkm4N|k>

... Click to View More Cell Line Experimental Data

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

Kinase Assay:

[1]

+ Expand

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 Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mice with human NCI-N87 gastric cancer xenograft.
  • Formulation: --
  • Dosages: 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.56 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 415.9
Formula

C19 H18 Cl N5 O2 S

CAS No. 959763-06-5
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID