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产品介绍
产品介绍
产品信息
抗原名称
PI3Kα；PI3Kδ；PI3Kβ；PI3Kγ
商品描述
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.
分子量
480.53
纯度
＞98%
可溶性
1M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)
DMSO : 1 mg/mL (2.08 mM; Need ultrasonic)
H2O : 0.67 mg/mL (1.39 mM; Need ultrasonic)
DMSO : 1 mg/mL (2.08 mM; Need ultrasonic)
H2O : 0.67 mg/mL (1.39 mM; Need ultrasonic)
外观
White powder
In vitro(体外研究)
In both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells.
In vivo(体内研究)
In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition.
背景
别名
库潘尼西；BAY 80-6946
分子式
C23H28N8O4
CAS号
1032568-63-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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