Copanlisib

製品コードS2802 バッチS280203

化学情報

	Synonyms	BAY 80-6946	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₃H₂₈N₈O₄
	分子量	480.52	CAS No.	1032568-63-0
Solubility (25°C)*	体外	5%TFA	3.78 mg/mL (7.86 mM)
		Ethanol	0.01 mg/mL (0.02 mM)
		DMSO	0.002 mg/mL (0.0 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Copanlisib is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
in vitro	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]
in vivo	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]

プロトコル(参考用のみ)

キナーゼアッセイ	Biochemical lipid kinase assays
キナーゼアッセイ	The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of ³³P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp® plates coated with 2 µg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 µL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl₂, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 µL of a 40-µM ATP solution containing 20 µCi/mL [^{33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 µL of a 25-mM EDTA solution. The plates are washed and Ultima Gold™ scintillation cocktail (25 µL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter.}
細胞アッセイ	細胞株	A series of cancer cell lines
	濃度	~5 μM
	反応時間	72 hours
	実験の流れ	Cell proliferation over a 72-hour period is determined using the CellTiter-Glo® luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37ºC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37ºC. Luminescence values are determined with a Wallac 1420 Victor2™ 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo® solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.
動物実験	動物モデル	Rats bearing KPL4 or HCT116 xenografts
	投薬量	6 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/24170767/
https://pubmed.ncbi.nlm.nih.gov/25528022/

カスタマーフィードバック

: , , Dr. Antonino Maria Spartà from University of Bolog

: , , Dr. Antonino Maria Spartà from University of Bolog

: Data from [Data independently produced by , , Oncol Rep, 2017, 37(5):3137-3145]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Deficiency in N-cadherin-Akt3 signaling impairs the blood-brain barrier [ Cell Rep, 2025, 44(6):115831]	PubMed: 40503940
KAT/3BP: A Metabolism-Targeting Agent with Single and Combination Activity in Aggressive B-Cell Lymphomas [ Cancers (Basel), 2025, 17(12)2034]	PubMed: 40563683
High Ano1 expression as key driver of resistance to radiation and cisplatin in HPV-negative head and neck squamous cell carcinoma [ Sci Rep, 2025, 15(1):1555]	PubMed: 39789065
Evaluation of co‑inhibition of ErbB family kinases and PI3K for HPV‑negative head and neck squamous cell carcinoma [ Oncol Rep, 2025, 53(3)38]	PubMed: 39886949
RHCG inhibition promotes the sensitivity of PIK3CA-mutant non-small lung cancer to PI3K inhibitor [ Histol Histopathol, 2025, 18946]	PubMed: 40509897
Exploiting an Epigenetic Resistance Mechanism to PI3 Kinase Inhibition in Leukemic Stem Cells [ bioRxiv, 2025, 2025.07.11.663968]	PubMed: 40791365
Longitudinal phosphoproteomics reveals the PI3K-PAK1 axis as a potential target for recurrent colorectal liver metastases [ Cell Rep, 2024, 43(12):115061]	PubMed: 39689713
Assessments of prostate cancer cell functions highlight differences between a pan-PI3K/mTOR inhibitor, gedatolisib, and single-node inhibitors of the PI3K/AKT/mTOR pathway [ Mol Oncol, 2024, 10.1002/1878-0261.13703]	PubMed: 39092562
Targeting CD25+ lymphoma cells with the antibody-drug conjugate camidanlumab tesirine as a single agent or in combination with targeted agents [ Br J Haematol, 2024, 10.1111/bjh.19658]	PubMed: 39080847
Functional Assessments of Gynecologic Cancer Models Highlight Differences Between Single-Node Inhibitors of the PI3K/AKT/mTOR Pathway and a Pan-PI3K/mTOR Inhibitor, Gedatolisib [ Cancers (Basel), 2024, 16(20)3520]	PubMed: 39456616

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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