中文名：TAS-116
英文名：TAS-116
纯度：Moligand™，≥98%
货号：T413821
Cas号：1260533-36-5
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
TAS-116 TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
Targets
HSP90β (Cell-free assay); HSP90α (Cell-free assay ) 21.3 nM(Ki); 34.7 nM(Ki)
In vitro
TAS-116 is a selective inhibitor of cytosolic HSP90α and β that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μmol/L TAS-116 for 8 hours results in reduced levels of DDR1, which interacts with HSP90α and induction of HSP70, which is a surrogate marker of cytosolic HSP90 inhibition.
In vivo
Oral administration of TAS-116 leads to tumor shrinkage in human tumor xenograft mouse models accompanied by depletion of multiple HSP90 clients. In a rat model, the antitumor activity of TAS-116 is accompanied by a higher distribution of the compound in subcutaneously xenografted NCI-H1975 non-small cell lung carcinoma tumors than in retina. TAS-116 shows activity against orthotopically transplanted NCI-H1975 lung tumors. Pharmacokinetic profiling of TAS-116 in rodent and nonrodent species shows that TAS-116 is orally absorbed and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation. In a HER2-expressing NCI-N87 human gastric cancer xenograft mouse model, chronic administration of TAS-116 is tolerable, with the average weight loss in mice not exceeding 10% during the treatment period.
Cell Research(from reference)
Cell lines：HCT116 cells
Concentrations：0.3, 1 and 3 μM
Incubation Time：8 hours
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/T413821.html
关键字： 3-Ethyl-4-(3-(1-methylethyl)-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo(3,4-b)pyridin-1-yl)benzamide ; HY-15785 ; DB14876 ; US8779142, 102
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代码：688179），专注于科研试剂的研发、生产和销售，已陆续建立多个工厂和研发中心。作为领军企业，阿拉丁始终坚持质量第一，连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种，SKU总数超过46万，产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域，是国内少数化学试剂到生物试剂全面发展的国产试剂品牌，产品同步发布在我们国内外电商平台。