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CH5138303

Catalog No. T6442   CAS 959763-06-5

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

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CH5138303 Chemical Structure
CH5138303, CAS 959763-06-5
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 649.00
1 mL * 10 mM (in DMSO) 6-8 weeks $ 225.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
Targets&IC50 HSP90α: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]
Kinase Assay 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 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)
Molecular Weight 415.9
Formula C19H18ClN5O2S
CAS No. 959763-06-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: <1 mg/mL

H2O: <1 mg/mL

DMSO: 77 mg/mL (185.1 mM)

TargetMolReferences and Literature

1. Suda A, et al. Bioorg Med Chem. 2014, 22(2), 892-905.

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Keywords

CH5138303 959763-06-5 Cytoskeletal Signaling Metabolism HSP gastric cancer inhibit CH-5138303 Inhibitor antitumor agent Hsp90 inhibitor orally active Heat shock proteins NCI-N87 CH 5138303 HCT116 inhibitor

 

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