品牌:JinPan | 货号:IC2980-2mg
可泮利塞
产品简介
CAS | 1032568-63-0 |
中文名称 | 可泮利塞 |
英文名称 | Copanlisib |
别名 | 库潘尼西 |
纯度 | ≥98% |
分子式 | C23H28N8O4 |
分子量 | 480.52 |
外观(性状) | Off-white to brown Solid |
储存条件 | Powder : 2-8℃, 2 years; In solvent(母液): -20℃, 1 month; -80℃, 6 months |
溶解性 | Soluble in Water ≥1mg/mL(Need to add HCl dropwise to help dissolve) |
MDL | MFCD18633201 |
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 |
SMILES | O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25 |
描述 | 是一种 ATP竞争,选择性 I 型 PI3K 抑制剂。(It is an ATP-competitive, selective type I PI3K inhibitor.) |
靶点 | PI3K |
通路 | PI3K/Akt/mTOR |
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 |
单位 | 瓶 |