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Borussertib-DataSheet-MedChemExpress.pdf

上传人:MedChemExpress 文档编号:439997 上传时间:2019-06-20 格式:PDF 页数:1 大小:92.12KB
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1、BorussertibCat. No.: HY-122913CAS No.: 1800070-77-2Molecular Formula: CHNOMolecular Weight: 596.68Target: AktPathway: PI3K/Akt/mTORStorage: Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITYDescription Borussertib is a covalent-allosteric and first-in-class inhi

2、bitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt1.IC & Target Aktwt0.8 nM (IC50)Aktwt2.2 nM (Ki)In Vitro Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic d

3、rug doxorubicin. The EC50 values are 19190 nM, 4815 nM, 51 nM, 27790 nM, 37354 nM, 7770641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively1.REFERENCES1. Niklas Uhlenbrock, et al. Structural and chemical insig

4、hts into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAProduct Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1

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