计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC 50 s 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
In Vitro
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. Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells. Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: BT20 breast cancer cells Concentration: 20 nM and 62 nM, 200 nM Incubation Time: 24 hours Result: Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC 50 of 340 nM. Western Blot AnalysisCell Line: ELT3 cells Concentration: 0.5 nM, 5 nM, 50 nM, 500 nM Incubation Time: 2 hours Result: Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nude rats injected with KPL4 tumor cells Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg Administration: Intravenous injection; every second day, every third day; for 60 days Result: On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.
IC50& Target:PI3Kα 0.5 nM (IC 50 ) PI3Kδ 0.7 nM (IC 50 ) PI3Kβ 3.7 nM (IC 50 ) PI3Kγ 6.4 nM (IC 50 ) mTOP 45 nM (IC 50 )
规格
别名
Copanlisib 二盐酸盐
规格或纯度
10mM in Water
英文名称
Copanlisib dihydrochloride
生化机理
Copanlisib dihydrochloride（BAY 80-6946 dihydrochloride）是一种强效、选择性和 ATP 竞争性泛 I 类 PI3K 抑制剂，对 PI3Kα 、PI3Kδ 、PI3Kβ 和 PI3Kγ 的 IC 50 s 分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。科潘利西二氢氯
储存条件
干燥,-80℃储存
运输条件
特低温运输
名称和识别符
EC号
815-039-6
分子类型
小分子
Isomeric SMILES
COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5.Cl.Cl
分子量
553.44
技术文档
高级数据
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1402152-13-9，分子式为 C23H30Cl2N8O4，分子量为 553.44 g/mol。
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