Home Cytoskeletal Signaling HSP (HSP90) inhibitor CH5138303 For research use only.

CH5138303

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

CH5138303 Chemical Structure

CH5138303 Chemical Structure

CAS: 959763-06-5

Purity & Quality Control

Batch: S734001 DMSO] 83 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.05%
99.05

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Signaling Pathway

HSP (HSP90) Signaling Pathways

HSP (HSP90) Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-N87 cells Cytotoxicity assay 4 days Cytotoxicity against human NCI-N87 cells after 4 days by CCk-8 assay, IC50=0.066 μM 24369839
HCT116 cells Cytotoxicity assay 4 days Cytotoxicity against human HCT116 cells after 4 days by CCk-8 assay, IC50=0.098 μM 24369839
NCI-N87 cells Function assay 0.04 to 5 uM 24 h Inhibition of Hsp90 in human NCI-N87 cells assessed as reduction in EGFR protein level at 0.04 to 5 uM after 24 hrs by Western blotting analysis 24369839
Click to View More Cell Line Experimental Data

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
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]
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 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.
In Vivo
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]
Animal Research Animal Models Mice with human NCI-N87 gastric cancer xenograft.
Dosages 50 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 415.9 Formula

C19 H18 Cl N5 O2 S
CAS No. 959763-06-5 SDF Download CH5138303 SDF
Smiles C1C2=C3C(=CC(=C(C3=CC=C2)C4=NC(=NC(=N4)SCCCC(=O)N)N)Cl)CO1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.56 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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