In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CH5138303 is an inhibitor of Hsp90 with Kd value of 0.48 nM .
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 .
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 .
. 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.
|Physical Appearance||A solid|
|Storage||Desiccate at -20°C|
|Formula||C19 H18 Cl N5 O2 S|
|Solubility||≥19.95mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||CH5138303 is an orally available inhibitor of Hsp90 with Kd value of 0.48 nM.|