An Hsp90 inhibitor (IC50 = 58 nM for recombinant human Hsp90β); selective for Hsp90 over GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM

NVP-BEP800 – 1 mg

Brand:
Cayman
CAS:
847559-80-2
Storage:
-20
UN-No:
Non-Hazardous - /

NVP-BEP800 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 58 nM for recombinant human Hsp90β).{29919} It is selective for Hsp90 over the chaperones GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively). NVP-BEP800 inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190, 173, and 162 nM, respectively). It reduces levels of the Hsp90 target proteins HER2 and Raf-1 in MCF-7 cells. NVP-BEP800 induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells.{29922} NVP-BEP800 (15-50 mg/kg) reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models.{29919} It also reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model.{29918}  

 

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Description

An Hsp90 inhibitor (IC50 = 58 nM for recombinant human Hsp90β); selective for Hsp90 over GRP94 and TRAP1 (IC50s = 4.1 and 5.5 µM, respectively); inhibits the growth of BT474, SK-BR-3, MCF-7, MDA-MB-157, MDA-MB-231, MDA-MB-468, and BT-20 breast cancer cells (GI50s = 53, 56, 118, 89, 190 173, and 162 nM, respectively); reduces levels of HER2 and Raf-1 in MCF-7 cells; induces apoptosis and attenuates X-ray-induced increases in Hsp70 levels in T98G glioblastoma cells; reduces tumor volume in A375 melanoma and BT474 breast cancer mouse xenograft models from 15-50 mg/kg; reduces tumor volume in an L1T2 Kaposi sarcoma mouse xenograft model

Formal name: 2-amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethyl-thieno[2,3-d]pyrimidine-6-carboxamide

Synonyms: 

Molecular weight: 480.4

CAS: 847559-80-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Cellular Chaperones

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