AZ10606120 dihydrochloride

製品コードS3520 バッチS352001

化学情報

	Synonyms	AZ10606120 2HCl	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₅H₃₆Cl₂N₄O₂
	分子量	495.48	CAS No.	607378-18-7
Solubility (25°C)*	体外	DMSO	99 mg/mL (199.8 mM)
		Water	17 mg/mL (34.31 mM)
		Ethanol	Insoluble
* <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	AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
in vitro	AZ10606120, a P2X7R antagonist, significantly reduces the tumour cell number in both U251 cells and human glioma samples, also more effectively inhibits tumour proliferation in U251 cells when compared with the conventional chemotherapeutic agent, temozolomide.^[2]
in vivo	AZ10606120, the P2X7R allosteric inhibitor, has anti‐proliferative effects in vivo, by reducing pancreatic stellate cells (PSCs) number/activity and collagen deposition.^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Glioma cells from human tumour sample , U251 human glioblastoma cell line
	濃度	5, 25 μM for U251 cells, 15 μM for human glioma samples
	反応時間	72 h
	実験の流れ	AZ10606120 concentrations of 5 μM and 25 μM was for U251 cells and 15 μM was for human glioma samples. For comparison of P2X7R antagonism efficacy with conventional glioma treatment, cells were also treated with the chemotherapeutic agent, temozolomide. After 72 h of treatment, cells were fixed with 1:1 acetone-methanol solution at − 20 °C for 15 min. Fixed cells were subsequently stained with 5 μM of DAPI nuclear counterstain at 25 °C for 1 h. Cells were viewed with an Olympus IX-81 fluorescence microscope, and a cell count was conducted based on the number of DAPI-positive nuclei.
動物実験	動物モデル	Orthotopic xenograft mouse model of pancreatic ductal adenocarcinoma (PDAC)
	投薬量	5 mg/kg
	投与方法	i.p.

参考

[1] Rebecca C Allsopp, et al. Sci Rep. 2017 Apr 7;7(1):725.
[2] Kan LK, et al. Purinergic Signal. 2020;16(3):327-336.
[3] Giannuzzo A, et al. Targeting of the P2X7 receptor in pancreatic cancer and stellate cells. Int J Cancer. 2016;139(11):2540-2552.

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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