VER-50589 是一种HSP90抑制剂，Kd值为 4.5 nM，IC50值为 21 nM。

VER-50589 is a potent HSP90 inhibitor.

在HCT116人结肠癌异种移植物中,VER-50589（100 mg/kg i.p.）导致肿瘤体积和重量约30％的统计学显著减少,以及HSP72的诱导和ERBB2和C-RAF的消耗.

VER-50589引起HSP72和HSP27的诱导伴随着客户蛋白（包括C-RAF,B-RAF和存活蛋白）和蛋白精氨酸甲基转移酶PRMT5的消耗,这进一步导致细胞周期停滞和细胞凋亡。VER-50589抑制重组酵母Hsp90的内在ATP酶活性,IC50为143 nM,并且在体外的一组人类癌细胞系和非肿瘤发生细胞中产生抗增殖活性。

Fluorescence Polarization Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.

Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method.(Only for Reference)

747413-08-7

C19H17ClN2O5

388.8

VER50589;5-(5-氯-2,4-二羟基苯基)-n-乙基-4-(4-甲氧基苯基)异噁唑-3-羧酰胺

H2O:<1 mgml
Ethanol:71 mg/mL (182.6 mM)
DMSO:71 mg/mL (182.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years