Copanlisib-dihydrochloride-BAY-80-6946-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECopanlisib dihydrochlorideCat. No.: HY-15346ACAS No.: 1402152-13-9Synonyms: BAY 80-6946 dihydrochloride分式: CHClNO分量: 553.44作靶点: PI3K作通路: PI3K/Akt/mTOR储存式: Please store the product under the recommended conditions inthe COA.BIOLO

2、GICAL ACTIVITY物活性 Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride)种有效的，选择性的和 ATP 竞争性的泛 I 类PI3K 抑制剂，对 PI3K，PI3K，PI3K 和 PI3K 的 IC50 分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除mTOR 外，Copanlisib dihydrochloride 对其他脂质和蛋激酶的选择性超过 2000 倍。Copanlisibdihydrochloride 具有优异的抗肿瘤活性。IC50 & Target PI3K PI3K PI3K PI3K

3、0.5 nM (IC50) 0.7 nM (IC50) 3.7 nM (IC50) 6.4 nM (IC50)mTOP45 nM (IC50)体外研究Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis ina subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab 1.Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hour

4、s; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells 1.Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against

5、 HER2-positive celllines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent 1.Apoptosis Analysis 1Cell Line: BT20 breast cancer cells1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEConcentration: 20 nM and 62 nM, 200 nMIncubation Time: 24 hoursResult: Sig

6、nificantly increased caspase9 activities. Also increased levels of phosphorylated p53at Ser15and cleaved PARP. Induced caspase-9 activation with an EC50 of 340 nM.Western Blot Analysis 1Cell Line: ELT3 cellsConcentration: 0.5 nM, 5 nM, 50 nM, 500 nMIncubation Time: 2 hoursResult: Complete inhibition

7、 of PI3K-mediated AKT phosphorylation was clearly shown at aconcentration of 5 nM.体内研究 Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days;athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model 1.A

8、nimal Model: Athymic nude rats injected with KPL4 tumor cells 1Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kgAdministration: Intravenous injection; every second day, every third day; for 60 daysResult: On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% wereobserved at doses of

9、 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free atthe termination of the study on day 73. Science. 2017 Dec 1;358(6367). Blood. 2019 Jan 3;133(1):70-80. Breast Cancer Res Treat. 2019 Oct 26. RSC Adv., 2019, 9, 6409-6418See more customer validations on HYPERLINK / www.MedChemEREFE

10、RENCES1. Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines andxenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: Product has not been fully valida