产品
编 号：F014543
分子式：C23H28N8O4
分子量：480.52
分子式：C23H28N8O4
分子量：480.52
产品类型
规格
价格
是否有货
2mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 1032568-63-0
产品详情
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.
体内研究：
Copanlisib (BAY 80-6946；0.5-6 mg/kg；静脉注射；每两天一次，每三天一次；持续 60 天；无胸腺裸鼠) 处理在大鼠 KPL4 肿瘤异种移植模型中显示出强大的抗肿瘤活性。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.
体外研究：
Copanlisib (BAY 80-6946；20 -200 nM；24 小时；BT20 乳腺癌细胞) 处理诱导对拉帕替尼和曲妥珠单抗耐药的肿瘤细胞系子集发生细胞凋亡。 Copanlisib (BAY 80-6946；0.5-500 nM；2 小时；ELT3 细胞) 处理显示完全抑制 ELT3 细胞中 PI3K 介导的 AKT 磷酸化。 Copanlisib 有效抑制一组人类肿瘤细胞系中的细胞增殖。Copanlisib 对具有 PIK3CA 激活突变的细胞系的平均 IC50 值为 19 nM，对 HER2 阳性细胞系的平均 IC50 值为 17 nM，而在 PIK3CA 野生型和HER2 阴性细胞的效力要低约 40 倍。
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.
体内研究：
Copanlisib (BAY 80-6946；0.5-6 mg/kg；静脉注射；每两天一次，每三天一次；持续 60 天；无胸腺裸鼠) 处理在大鼠 KPL4 肿瘤异种移植模型中显示出强大的抗肿瘤活性。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.
体外研究：
Copanlisib (BAY 80-6946；20 -200 nM；24 小时；BT20 乳腺癌细胞) 处理诱导对拉帕替尼和曲妥珠单抗耐药的肿瘤细胞系子集发生细胞凋亡。 Copanlisib (BAY 80-6946；0.5-500 nM；2 小时；ELT3 细胞) 处理显示完全抑制 ELT3 细胞中 PI3K 介导的 AKT 磷酸化。 Copanlisib 有效抑制一组人类肿瘤细胞系中的细胞增殖。Copanlisib 对具有 PIK3CA 激活突变的细胞系的平均 IC50 值为 19 nM，对 HER2 阳性细胞系的平均 IC50 值为 17 nM，而在 PIK3CA 野生型和HER2 阴性细胞的效力要低约 40 倍。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备