PF-06424439

製品コードS9921 バッチS992101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₃H₃₀ClN₇O₄S

分子量

536.05

CAS No.

1469284-79-4

Solubility (25°C)*

体外

DMSO

88 mg/mL (164.16 mM)

Water

88 mg/mL (164.16 mM)

Ethanol

88 mg/mL (164.16 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.55mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM.
in vitro	PF-06424439 treatment reduces LD content and inhibites cell migration, without affecting cell proliferation. PF-06424439 pre-treatment followed by radiation can enhance radiosensitivity of MCF7 cells.<sup><a class="sref" href="#s_ref">[2]</a></sup>
in vivo	PF-06424439 reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-). PF-06424439 shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life.<sup><a class="sref" href="#s_ref">[1]</a></sup>

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MCF-7 cells
	濃度	1, 10, 50, 100, 200 μM
	反応時間	24, 48, 72, and 96 h
	実験の流れ	MCF7 cells are seeded at 4.7 × 10<sup>3</sup> cells/well in 96-well black polystyrene microplates and incubated overnight at 37 °C to allow for cell attachment. The next day, cells are treated with 1, 10, 50, 100, 200 μM of PF-06424439 for 24, 48, 72, and 96 h, and then used for Cell Viability Assay by Presto Blue Cell Viability Reagent. Cells are seeded in 100 mm dishes, incubated overnight at 37 °C and then treated with 10 μM of PF-06424439 for 72 h. Subsequently, cells are collected for clonogenic survival assay, cell death detection, cell cycle analysis, γ-H2AX staining,and lipid droplets staining.<sup><a class="sref" href="#s_ref">[2]</a></sup>
動物実験	動物モデル	Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
	投薬量	60 mg/kg
	投与方法	p.o., i.v.

参考

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。