Copanlisib
Cat. No.:YN420209
产品名称: | Copanlisib |
CAS No.: | 1032568-63-0 |
Chemical Name: | 2-amino-N-[2,3-dihydro-7-methoxy-8-[3-(4-morpholinyl)propoxy]imidazo[1,2-c]quinazolin-5-yl]-5-pyrimidinecarboxamide |
Synonyms: | 库潘尼西; BAY 80-6946 |
分子量: | 480.52 |
分子式: | C₂₃H₂₈N₈O₄ |
SMILES: | O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Copanlisib (BAY 80-6946) 是一种有效的,选择性的和 ATP 竞争性的泛 I 类PI3K抑制剂,对PI3Kα,PI3Kδ,PI3Kβ和PI3Kγ的IC50分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除 mTOR 外,Copanlisib 对其他脂质和蛋白激酶的选择性超过 2000 倍。Copanlisib 具有优异的抗肿瘤活性。 |
IC50和靶点: | [{name:"PI3Kα:0.5 nM (IC50)"},{name: "PI3Kδ:0.7 nM (IC50)"},{name: "PI3Kβ:3.7 nM (IC50)"},{name: "PI3Kγ:6.4 nM (IC50)"},{name: "mTOR:45 nM (IC50)"}] |
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Liu, N., Rowley, B.R., Bull, C.O., et al.BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft modelsMol. Cancer Ther.12(11),2319-2330(2013)
Will, M., Qin, A.C.R., Toy, W., et al.Rapid induction of apoptosis by PI3K inhibitors is dependent upon their transient inhibition of RAS-ERK signalingCancer Discov.4(3),334-347(2014)