产品描述:PRQ620 is a highly potent and selective mTORC1/2 inhibitor, shows anti-tumor effects in vitro and in vivo.
target: mTORC1/2
IC 50: 0.2 μM and 0.1 μM.
In vitro: In A2058 melanoma cells PQR620 demonstrated inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50values of 0.2 μM and 0.1 μM, respectively. PQR620 demonstrated its potency to prevent cancer cell growth in an NTRC 44 cancer cell line panel, resulting in a 10log(IC50) of 2.86 (nM), induced a >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays. showed excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. [1]
In vivo: PQR620 result in good oral bioavailability and excellent brain penetration. [1]
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。
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