847559-80-2 Usage
Description
NVP-BEP800 is a Hsp90 inhibitor, a type of compound that targets the heat shock protein 90 (Hsp90) to exhibit anti-proliferative effects against cancer cell lines with high expression levels of Hsp90.
Uses
Used in Pharmaceutical Industry:
NVP-BEP800 is used as an anti-cancer agent for its ability to inhibit the Hsp90 protein, which is often overexpressed in cancer cells. This inhibition can lead to the suppression of tumor growth and the prevention of cancer progression.
Used in Cancer Research:
NVP-BEP800 is utilized in cancer research as a tool to study the role of Hsp90 in various types of cancer and to investigate the potential of Hsp90 inhibitors as therapeutic agents for cancer treatment.
Used in Drug Development:
NVP-BEP800 serves as a lead compound in the development of new drugs targeting the Hsp90 protein, with the aim of creating more effective and targeted cancer treatments.
Biological Activity
nvp-bep800 is a fully synthetic, orally bioavailable inhibitor of hsp90 with ic50 value of 58nm [1].nvp-bep800 binds to the n-terminal atp-binding pocket of hsp90. in a competitive binding fluorescence polarization assay, nvp-bep800 inhibits hsp90β with ic50 value of 58nm. and to other 20 protein kinases, nvp-bep800 shows a ic50 of >10μm. 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. nvp-bep800 inhibits proliferation of tumor cells with an average gi50 of 245nm. and in 46 primary human tumors including small cell lung, mammary cancer and melanoma, the mean ic50 is 750nm. additionally, treatment of nvp-bep800 induces apoptosis in human breast cancer cell lines. the antitumor efficacy of nvp-bep800 is also observed with a dose of 15 or 30 mg/kg/d in a375 xenograft-bearing mice as well as in bt-474 breast cancer xenografts [1].
references
[1] massey aj, schoepfer j, brough pa, brueggen j, chène p, drysdale mj, pfaar u, radimerski t, ruetz s, schweitzer a, wood m, garcia-echeverria c, jensen mr. preclinical antitumor activity of the orally available heat shock protein 90 inhibitor nvp-bep800. mol cancer ther. 2010 apr;9(4):906-19.
Check Digit Verification of cas no
The CAS Registry Mumber 847559-80-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,4,7,5,5 and 9 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 847559-80:
(8*8)+(7*4)+(6*7)+(5*5)+(4*5)+(3*9)+(2*8)+(1*0)=222
222 % 10 = 2
So 847559-80-2 is a valid CAS Registry Number.
847559-80-2Relevant articles and documents
Combining hit identification strategies: Fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone
Brough, Paul A.,Barril, Xavier,Borgognoni, Jenifer,Chene, Patrick,Davies, Nicholas G. M.,Davis, Ben,Drysdale, Martin J.,Dymock, Brian,Eccles, Suzanne A.,Garcia-Echeverria, Carlos,Fromont, Christophe,Hayes, Angela,Hubbard, Roderick E.,Jordan, Allan M.,Jensen, Michael Rugaard,Massey, Andrew,Merrett, Angela,Padfield, Antony,Parsons, Rachel,Radimerski, Thomas,Raynaud, Florence I.,Robertson, Alan,Roughley, Stephen D.,Schoepfer, Joseph,Simmonite, Heather,Sharp, Swee Y.,Surgenor, Allan,Valenti, Melanie,Walls, Steven,Webb, Paul,Wood, Mike,Workman, Paul,Wright, Lisa
supporting information; experimental part, p. 4794 - 4809 (2010/03/01)
Inhibitors of the Hsp90 molecular chaperone are showing considerable promise as potential molecular therapeutic agents for the treatment of cancer. Here we describe novel 2-aminothieno[2,3-d]pyrimidine ATP competitive Hsp90 inhibitors, which were designed
