可泮利塞

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.
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