Copanlisib dihydrochloride |
رقم الكتالوجGC60112 |
ثنائي هيدروكلوريد كوبانليسيب (BAY 80-6946 ثنائي هيدروكلوريد) هو مثبط قوي وانتقائي وتنافسي ATP من الفئة I PI3K ، مع IC50s من 0.5 نانومتر و 0.7 نانومتر و 3.7 نانومتر و 6.4 نانومتر لـ PI3Kα و PI3Kδ و PI3Kβ و PI3Kγ ، على التوالييحتوي ثنائي هيدروكلوريد كوبانليسيب على أكثر من 2000 ضعف انتقائية ضد كينازات الدهون والبروتينات الأخرى ، باستثناء mTORثنائي هيدروكلوريد كوبانليسيب له نشاط مضاد للأورام متفوق
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Cas No.: 1402152-13-9
Sample solution is provided at 25 µL, 10mM.
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity[1].
Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1].Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; 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 IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[1]. Apoptosis Analysis[1] Cell Line: BT20 breast cancer cells
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]. Animal Model: Athymic nude rats injected with KPL4 tumor cells[1]
[1]. Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30.
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