
NSC139021
CAS No. 1147-56-4
NSC139021 ( ERGi-USU )
产品货号. M20631 CAS No. 1147-56-4
NSC139021 是一种 Rio2 激酶 (RIOK2) 抑制剂,可抑制 ERG 蛋白。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
100MG | ¥332 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称NSC139021
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注意事项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
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产品简述NSC139021 是一种 Rio2 激酶 (RIOK2) 抑制剂,可抑制 ERG 蛋白。
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产品描述NSC139021 is a Rio2 kinase (RIOK2) inhibitor that inhibits ERG protein.
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体外实验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.
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体内实验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. .
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同义词ERGi-USU
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通路Others
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靶点Other Targets
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受体Rio2 kinase (RIOK2)
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研究领域——
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适应症——
化学信息
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CAS Number1147-56-4
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分子量255.3
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分子式C13H9N3OS
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纯度>98% (HPLC)
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溶解度DMSO:62 mg/mL (242.85 mM)
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SMILESOc1ccc2ccccc2c1N=Nc1nccs1
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化学全称1-[2-(2-Thiazolyl)diazenyl]-2-naphthalenol
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Mohamed A A Xavier C P Sukumar G et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth[J]. Cancer Research 2018:canres.2949.2017.
产品手册




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