PHY34

製品コードS8744 バッチS874401

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₀H₃₀O₁₂
	分子量	582.55	CAS No.	2130033-55-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (171.65 mM)
		Ethanol	42 mg/mL (72.09 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	PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
in vitro	PHY34 is a cytotoxic compound in both HGSOC cell lines with an IC50 of 4 nM. It has nanomolar IC50s in both MDA-MB-435 and MDAMB-231 cell lines and is more cytotoxic against MDA-MB-231 (PHY34 IC50 in MDA-MB-435 = 23 nM, PHY34 IC50 in MDA-MB-231 = 5.2 nM). PHY34 treatment (100 nM) results in significant increases in early and late apoptotic cells in OVCAR3^[1].
in vivo	PHY34 is bioavailable through intraperitoneal administration in vivo where it significantly inhibits the growth of cancer cell lines in hollow fibers, as well as reduces ovarian tumor burden in a xenograft model. Mice are dosed with 0.6 mg/kg IV, 1.8 mg/kg IP, or 75 mg/kg PO PHY34, the observed IP bioavailability (F) for PHY34 is 56.6% and for PO is 2.5%. Systemic clearance (Cl) following PO dose is 194.1 L/hr/kg, roughly 40 times the mouse liver blood flow, suggesting significant extrahepatic clearance. The Tmax of PHY34 (0.25 hr) suggests very fast absorption of this compound orally. PHY34 reduces tumor burden (OVCAR8 cells) in vivo^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	OVCAR8 and OVCAR3 cells
	濃度	100 nM or 1 μM
	反応時間	24 h
	実験の流れ	OVCAR8 and OVCAR3 cells are treated with PHY34 for 24 hours at 100 nM or 1 μM, respectively, and stained with either Lysotracker Red or acridine orange to monitor changes in the lysosomes due to autophagy inhibition using live confocal microscopy.
動物実験	動物モデル	ICR male mice (6 weeks in age)
	投薬量	3, 1, 0.6 and 0.3 mg/kg
	投与方法	i.v.

参考

[1] Young AN, et al. Mol Cancer Ther. 2018, 17(10):2123-2135.

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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