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CH5138303

Catalog No.
B4571
Hsp90 inhibitor, orally available
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$280.00
In stock
1mg
$67.00
In stock
5mg
$237.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

CH5138303 is an inhibitor of Hsp90 with Kd value of 0.48 nM [1].

Heat shock protein 90 (HSP90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. Also, HSP90 stabilizes proteins required for tumor growth.

CH5138303 is an orally available Hsp90 inhibitor. CH5138303 showed improved water solubility with 646 μM and high affinity against Hsp90α with Kd value of 0.48 nM. In NCI-N87 cells, CH5138303 decreased the protein level and phosphorylation of Hsp90 target proteins such as Raf1, AKT, EGFR and HER2 [1].

In mice, CH5138303 exhibited high plasma clearance, oral bioavailability and total systemic exposure (AUC). In mice bearing human NCI-N87 gastric cancer xenograft model, CH5138303 exhibited potent antitumor efficacy with tumor growth inhibition (TGI) of 136% and ED50 value of 3.9 mg/kg [1].

Reference:
[1].  Suda A, Kawasaki K, Komiyama S, et al. Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorg Med Chem, 2014, 22(2): 892-905.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt415.9
Cas No.959763-06-5
FormulaC19 H18 Cl N5 O2 S
Solubility≥19.95mg/mL in DMSO
SDFDownload SDF
Canonical SMILESClC1=C(C2=NC(N)=NC(SCCCC(N)=O)=N2)C3=CC=CC4=C3C(COC4)=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description CH5138303 is an orally available inhibitor of Hsp90 with Kd value of 0.48 nM.
Targets Hsp90          
IC50 (Kd=0.48 nM)          

Quality Control

Quality Control & MSDS

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Chemical structure

CH5138303