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Copanlisib dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Copanlisib dihydrochloride图片
CAS NO:1402152-13-9
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
库潘尼西盐酸
BAY 80-6946 dihydrochloride
产品介绍
Copanlisib dihydrochloride 是一种选择性和 ATP 竞争性的泛 I 类PI3K抑制剂。它具有优越的抗肿瘤活性,对除 mTOR 以外的其他脂质和蛋白激酶的选择性也超过 2,000 倍。

产品描述

Copanlisib dihydrochloride is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ). Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

体外活性

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. [1] 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. [2]

体内活性

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. [1]

Cas No.

1402152-13-9

分子式

C23H30Cl2N8O4

分子量

553.45

别名

库潘尼西盐酸;BAY 80-6946 dihydrochloride

储存和溶解度

H2O:20mg/mL,Need ultrasonic
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years