An HSP90 inhibitor (IC50 = 10 nM in a fluorescence polarization assay); decreases HER2 protein expression (IC50 = 110 nM) in BT474 breast cancer cells; inhibits the growth of a 16 cancer cell line panel (IC50s = 13-362 nM); reduces tumor growth by 74% in an A2780 mouse xenograft model at a dose of 60 mg/kg

NMS-E973 – 5 mg

Brand:
Cayman
CAS:
1253584-84-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

NMS-E973 is an inhibitor of heat shock protein 90 (HSP90; IC50 = 10 nM in a fluorescence polarization assay).{37249} It decreases HER2 protein expression (IC50 = 110 nM) in BT474 breast cancer cells and inhibits the growth of a 16 cancer cell line panel (IC50s = 13-362 nM).{37249},{37250} NMS-E973 (60 mg/kg, i.v., per day for ten days) reduces tumor growth by 74% in an A2780 xenograft mouse model. It reduces expression of HSP90 client proteins, phosphorylated ERK and AKT, and total AKT in lysates from A2780 tumors. NMS-E973 also completely eradicates MOLM-13 acute myeloid leukemia tumors in a mouse xenograft model.{37250}  

 

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Description

An HSP90 inhibitor (IC50 = 10 nM in a fluorescence polarization assay); decreases HER2 protein expression (IC50 = 110 nM) in BT474 breast cancer cells; inhibits the growth of a 16 cancer cell line panel (IC50s = 13-362 nM); reduces tumor growth by 74% in an A2780 mouse xenograft model at a dose of 60 mg/kg, i.v., per day for ten days; completely eradicates MOLM-13 acute myeloid leukemia tumors in a mouse xenograft model

Formal name: 5-[2,4-dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide

Synonyms: 

Molecular weight: 454.4

CAS: 1253584-84-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cellular Chaperones

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