Acelarin (NUC-1031)

製品コードS9649 バッチS964901

化学情報

	Synonyms	CPF-31, MTL-007, GTPL7389	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₅H₂₇F₂N₄O₈P
	分子量	580.47	CAS No.	840506-29-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (172.27 mM)
		Ethanol	20 mg/mL (34.45 mM)
		Water	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	Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
in vitro	NUC-1031 is a prodrug with potent cytostatic activity in a range of different tumor cell lines. Importantly, NUC-1031 activation is significantly less dependent on deoxycytidine kinase and on nucleoside transporters, and it is resistant to cytidine deaminase-mediated degradation.^[1]
in vivo	NUC-1031 shows a significant reduction in tumor volumes in vivo in pancreatic cancer xenografts.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Murine leukemia L1210, human lymphocyte CEM
	濃度	1 μM
	反応時間	1 h
	実験の流れ	Metabolic Stability (Cryopreserved Hepatocytes, Human) Assay. The assay is contracted and performed by Cerep according to the published procedure.Pooled cryopreserved hepatocytes are thawed, washed, and resuspended in Krebs-Heinslet buffer (pH 7.3). The reaction is initiated by adding Acelarin (NUC-1031) (1 μM final concentration) into cell suspension and incubated in a final volume of 100 μL on a flatbottom 96-well plate for 0 and 60 min, respectively, at 37 ℃/5% CO2. The reaction is stopped by adding 100 μL of acetonitrile into the incubation mixture. Samples are then mixed gently and briefly on a plate shaker, transferred completely to a 0.8 mL V-bottom 96-well plate, and centrifuged at 2550 × g for 15 min at room temperature. Each supernatant (150 μL) is transferred to a clean cluster tube, followed by HPLC-MS/MS analysis on a Thermo Electron triplequadrupole system.
動物実験	動物モデル	MiaPaCa-2 bearing nude mice, BxPC-3 bearing nude mice
	投薬量	0.19 mM/kg, 0.076 mM/kg
	投与方法	IP

参考

[1] Magdalena Slusarczyk, et al. J Med Chem. 2014 Feb 27;57(4):1531-42.

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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