NVP-BEP800
Catalog #
27766-1
$260
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Description
NVP-BEP800 is a novel, fully synthetic, oral inhibitor of Hsp90β with IC50 value of 58 nM.
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Synonyms
VER-82576; 2-amino-4-[2,4-dichloro-5-(2-pyrrolidin-1-ylethoxy)phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
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Product Data Gallery
Chemical Structure
Product Info
Storage and Usage
Citations
Purity
≥99%
Format
Solid
Target(s)
Hsp90β
Formula
C21H23Cl2N5O2S
MW
480.4 Da
Solubility
≥16 mg/ml in EtOH with gentle warming; ≥24.7 mg/mL in DMSO with gentle warming and ultrasonic; insoluble in H2O. For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Long-term storage in solution is not recommended. Not stable in diluted solutions.
CAS Registry #
847559-80-2
Background
NVP-BEP800 binds to the N-terminal ATP-binding pocket of Hsp90. Hsp90 is a ubiquitously expressed molecular chaperone with ATPase activity involved in the conformational maturation and stability of key signaling molecules involved in cell proliferation, survival, and transformation. In BT-474 cells and A375 cells, NVP-BEP800 causes the Hsp90-p23 dissociation and client protein degradation (ErbB2) as well as the reduction of client protein phosphorylation (phospho-Akt). Degradation of these oncogenic client proteins results in tumor cell growth arrest and death.
References
Massey AJ, et al. Mol Cancer Ther. 2010 Apr;9(4):906-19.
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