NSC139021

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSC139021 是一种 Rio2 激酶 (RIOK2) 抑制剂，可抑制 ERG 蛋白。

NSC139021 is a Rio2 kinase (RIOK2) inhibitor that inhibits ERG protein.

NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines. The IC50 of NSC139021 for cell growth inhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 with enzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal that NSC139021 directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induces ribosomal stress signature.

NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity. Significant (P<0.05, P<0.005) inhibition of tumor growth is noted at day 26 in treatment groups indicating 44% (100 mg/kg) and 65% (150 mg/kg) reduction of tumor burden. At 100 mg/kg and 150 mg/kg, no apparent toxicity including weight loss, lethargy, diarrhea, loss of appetite, respiratory distress, or overall drug related toxicity is observed. .

ERGi-USU

Others

Other Targets

Rio2 kinase (RIOK2)

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1147-56-4

255.3

C13H9N3OS

>98% (HPLC)

DMSO:62 mg/mL (242.85 mM)

Oc1ccc2ccccc2c1N=Nc1nccs1

1-[2-(2-Thiazolyl)diazenyl]-2-naphthalenol

(-20℃)

With Ice Pack

≥ 2 years