Copanlisib (BAY 80-6946) | PI3K inhibitor | Probechem Biochemicals

Chemical Structure : Copanlisib

CAS No.: 1032568-63-0

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Copanlisib (BAY 80-6946, BAY80-6946)

货号: PC-20534Not For Human Use, Lab Use Only.

Copanlisib (BAY 80-6946) is a potent, highly selective pan-class I PI3K inhibitor with IC50 of 0.5, 3.7, 6.4, and 0.7 nM for PI3Kα, β, γ, and δ isoforms, respectively.

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5 mg	￥880	In stock
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg		Get quote

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生物&药学活性

Copanlisib (BAY 80-6946) is a potent, highly selective pan-class I PI3K inhibitor with IC50 of 0.5, 3.7, 6.4, and 0.7 nM for PI3Kα, β, γ, and δ isoforms, respectively.
BAY 80-6946 shows significantly weaker activity against mTOR with an IC50 of 45 nM, does not inhibit PI4K-II, PIP4-5K, PIP5-4K, or an additional 220 kinases in the Millipore kinase panel (inhibition <30%) at 1 uM.
BAY 80-6946 reduces basal levels of AKT phosphorylation at both Thr308 and Ser473 with IC50 values of 0.4 and 0.6 nmol/L, respectively, in KPL4 cells.
BAY 80-6946 is a potent inhibitor of tumor cell proliferation and shows activity in a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2.
BAY 80-6946 induces apoptosis in a subset of tumor cell lines that are resistant to lapatinib and trastuzumab.
BAY 80-6946 is highly efficacious in rat and mouse tumor xenograft models following intravenous administration.

物理化学性质&存储条件

分子量	480.53
分子式	C23H28N8O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-amino-N-(7-methoxy-8-(3-morpholinopropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyrimidine-5-carboxamide

参考文献

1. Liu N, et al. Mol Cancer Ther. 2013 Nov;12(11):2319-30.

2. Will M, et al. Cancer Discov. 2014 Mar;4(3):334-47.

Copanlisib (BAY 80-6946, BAY80-6946)

生物&药学活性

物理化学性质&存储条件

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Copanlisib (BAY 80-6946, BAY80-6946)

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物理化学性质&存储条件

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