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NSC 663284前沿研究进展
507 人阅读发布时间：2018-06-29 14:56
NSC 663284产品描述：NSC 663284是 Cdc25 双重特异性磷酸酶抑制剂， IC50 值为0.21 μM。
NSC 663284产品描述：NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.IC50 & Target: IC50: 0.21 μM (Cdc25 dual specificity phosphatase)[1]In Vitro: The Cdc25 dual specificity phosphatases have central roles in coordinating cellular signaling processes and cell proliferation. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B2, and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 blocks cellular Erk dephosphorylation caused by ectopic Cdc25A expression. NSC 663284 displays a strong preference for Cdc25B2 as compared with VHR or PTP1B, the relative IC50 values for Cdc25B2 are 20- and 450-fold lower than for VHR or PTP1B, respectively. NSC 663284 blocks cell proliferation and the actions of cellular cdc25a. NSC 663284 has a mean IC50 value in the NCI 60 Cell Human Tumor Panel of 1.5 (0.6 µM when cells are treated for 48 h). Most sensitive are human breast cancer MDA-MB-435 and MDA-N cells, which have IC50 values of 0.2 µM[1].In Vivo: NSC 663284 inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single i.v. dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys[2].
研究领域：Anti-infection
靶点：HIV
相关产品：Dolutegravir | Maraviroc | Elvitegravir | Atazanavir sulfate | Tenofovir Disoproxil Fumarate | Tipranavir | Triciribine | Emtricitabine | Efavirenz | Miltefosine | Ritonavir | Delavirdine mesylate | Lamivudine | Abacavir | BI 224436 |
Alternative_Names:DA-3003-1
MWt:321.76
Formula:C15H16ClN3O3
SMILES:O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O
Research_Area:Cancer
公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、专利；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足最新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
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网址：www.medchemexpress.cn
地址:上海市浦东新区蔡伦路720号2号楼5层
NSC 663284产品描述：NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.IC50 & Target: IC50: 0.21 μM (Cdc25 dual specificity phosphatase)[1]In Vitro: The Cdc25 dual specificity phosphatases have central roles in coordinating cellular signaling processes and cell proliferation. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B2, and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 blocks cellular Erk dephosphorylation caused by ectopic Cdc25A expression. NSC 663284 displays a strong preference for Cdc25B2 as compared with VHR or PTP1B, the relative IC50 values for Cdc25B2 are 20- and 450-fold lower than for VHR or PTP1B, respectively. NSC 663284 blocks cell proliferation and the actions of cellular cdc25a. NSC 663284 has a mean IC50 value in the NCI 60 Cell Human Tumor Panel of 1.5 (0.6 µM when cells are treated for 48 h). Most sensitive are human breast cancer MDA-MB-435 and MDA-N cells, which have IC50 values of 0.2 µM[1].In Vivo: NSC 663284 inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single i.v. dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys[2].
研究领域：Anti-infection
靶点：HIV
相关产品：Dolutegravir | Maraviroc | Elvitegravir | Atazanavir sulfate | Tenofovir Disoproxil Fumarate | Tipranavir | Triciribine | Emtricitabine | Efavirenz | Miltefosine | Ritonavir | Delavirdine mesylate | Lamivudine | Abacavir | BI 224436 |
Alternative_Names:DA-3003-1
MWt:321.76
Formula:C15H16ClN3O3
SMILES:O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O
Research_Area:Cancer
公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、专利；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足最新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供免费试用装； 已为全球多个知名企业、院校构建各种定制型化合物库。
电话:021-58955997
网址：www.medchemexpress.cn
地址:上海市浦东新区蔡伦路720号2号楼5层