NMS-E973 - 10mM in DMSO, high purity , CAS No.1253584-84-7

Item Number

N421061

• Synonyms: NMS-E973 | 1253584-84-7 | 5-[2,4-Dihydroxy-6-(4-Nitrophenoxy)phenyl]-N-(1-Methylpiperidin-4-Yl)-1,2-Oxazole-3-Carboxamide | CHEMBL2443044 | SCHEMBL657965 | NMS E973 | NMS-973 | NMSE973; NMS E973 | HMS3653E08 | BCP29502 | EX-A4406 | BDBM50442760 | s7282 | AKOS027307871 | CCG-269277 | S
• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

NMS-E973 NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.

Targets

HSP90 <10 nM(DC50)

In vitro

NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways.

In vivo

NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90.

Cell Research(from reference)

Cell lines：140 human tumor cell lines of various tissue origins and molecular background. 

Concentrations：~10 μM