ERGi-USU (NSC139021)

Chemical Structure : ERGi-USU

CAS No.: 1147-56-4

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货号: PC-63456Not For Human Use, Lab Use Only.

ERGi-USU (NSC 139021) is a specific RIOK2 inhibitor, selectively inhibits ERG-positive cancer cell growth, directly binds (Kd=200 nM) and inhibits RIOK2 protein with IC50 of 220 nM (VCaP) and 360 nM (COLO320).

规格	价格	库存
100 mg	￥480	In stock
250 mg	￥780	In stock
1 g		Get quote

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生物&药学活性

ERGi-USU (NSC 139021) is a specific RIOK2 inhibitor, selectively inhibits ERG-positive cancer cell growth, directly binds (Kd=200 nM) and inhibits RIOK2 protein with IC50 of 220 nM (VCaP) and 360 nM (COLO320).

ERGi-USU selectively inhibited growth of ERG-positive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines.

Combination of ERGi-USU with enzalutamide showed additive effects in inhibiting growth of VCaP cells.

ERGi-USU directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induced ribosomal stress signature.

ERGi-USU treatment inhibited growth of ERG-positive VCaP tumor xenografts with no apparent toxicity.

ERGi-USU acts as a highly selective inhibitor for the growth of ERG-positive cancer cells and has potential for further development of ERG-targeted therapy of prostate cancer and other malignancies.

物理化学性质&存储条件

分子量	255.295
分子式	C13H9N3OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-[2-Thiazolylazo]-2-naphthol

参考文献

1. Mohamed AA, et al. Cancer Res. 2018 Apr 30. pii: canres.2949.2017.