An Hsp90 inhibitor (IC50s = 0.6

HSP-990 – 25 mg

Brand:
Cayman
CAS:
934343-74-5
Storage:
-20
UN-No:
Non-Hazardous - /

The heat shock proteins (Hsps) act as molecular chaperones. Hsp90 is an abundant protein with roles in protein folding, cell signaling, and cancer. HSP-990 is an Hsp90 inhibitor with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and GRP94, respectively.{31009} It inhibits the TRAP1 ATPase with an IC50 value of 320 nM and demonstrates IC50 values of >5 µM in a panel of 51 unrelated kinases.{31009} In c-Met amplified GTL-16 gastric tumor cells, HSP-990 has been shown to dissociate the Hsp90-p23 complex, depleting the client protein c-Met and inducing Hsp70.{31009} HSP-990 can inhibit proliferation of various human tumor cell lines with GI50 values of 4-40 nM.{31009} Single oral administration of 15 mg/kg of HSP-990 was shown to induce sustained downregulation of c-Met and upregulation of Hsp70 in a GTL-16 xenograft model.{31009}  

 

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Description

An Hsp90 inhibitor (IC50s = 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and GRP94, respectively); dissociates the Hsp90-p23 complex, depleting the client protein c-Met and inducing Hsp70 in c-Met amplified GTL-16 gastric tumor cells; inhibits proliferation of various human tumor cell lines in vitro and in a GTL-16 xenograft model

Formal name: (7R)-2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-pyrido[4,3-d]pyrimidin-5(6H)-one

Synonyms:  ​NVP-HSP990

Molecular weight: 379.4

CAS: 934343-74-5

Purity: ≥98%

Formulation: A crystalline solid

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

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