| CAS |
No.1032568-63-0 |
| 中文名称 |
可泮利塞 |
| 英文名称 |
Copanlisib |
| 别名 |
库潘尼西 |
| 分子式 |
C23H28N8O4 |
| 分子量 |
480.52 |
| 溶解性 |
Soluble in Water ≥1mg/mL(Need to add HCl dropwise to help dissolve) |
| 纯度 |
≥98% |
| 外观(性状) |
Off-white to brown Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| MDL |
MFCD18633201 |
| SMILES |
O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25 |
| InChIKey |
MWYDSXOGIBMAET-UHFFFAOYSA-N |
| InChI |
InChI=1S/C23H28N8O4/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15/h3-4,13-14,25H,2,5-12H2,1H3,(H2,24,26,27) |
| PubChem CID |
135565596 |
| 靶点 |
PI3K |
| 通路 |
PI3K/Akt/mTOR |
| 背景说明 |
是一种 ATP竞争,选择性 I 型 PI3K 抑制剂。 |
| 生物活性 |
Copanlisib (BAY 80-6946) 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 has more than 2，000-fold selectivity against other lipid and protein kinases， except for mTOR. Copanlisib has superior antitumor activity[1]. |
| 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[1]. |
| 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[1]. |
| 数据来源文献 |
[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. |
| 规格 |
2mg 5mg 10mg 50mg 100mg |
| 单位 |
瓶 |
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英语
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