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VER-50589

VER-50589 是一种 Hsp90抑制剂，Kd 值为 4.5 nM，IC50值为 21 nM。

CAS号

747413-08-7

分子式

C19H17ClN2O5

主要靶点

Apoptosis|HSP

仅限科研使用

Cat No : CM04664

Print datasheet

Synonyms

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|VER50589

验证数据展示

  • CAS No.: 747413-08-7

    VER-50589
    CAS#: 747413-08-7

产品信息

VER-50589 is a potent HSP90 inhibitor.

CAS号 747413-08-7
分子式 C19H17ClN2O5
主要靶点 Apoptosis|HSP
主要通路 凋亡|代谢|细胞骨架
分子量 388.8
纯度 99.85%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 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|VER50589

靶点活性

HSP90β:21 nM

体内活性

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。

体外活性

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.

溶解度

DMSO:71 mg/mL (182.6 mM),H2O:<1 mg/mL,Ethanol:71 mg/mL (182.6 mM)

细胞实验

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

参考文献

1.Sharp SY, et al. Mol Cancer Ther. 2007, 6(4), 1198-1211.

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