PF-4989216

製品コードS7675 バッチS767501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₃FN₆OS

分子量

380.4

CAS No.

1276553-09-3

Solubility (25°C)*

体外

DMSO

76 mg/mL (199.78 mM)

Ethanol (warmed with 50ºC water bath)

7 mg/mL (18.4 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

Suspended in 0.5% methylcellulose

1.0mg/ml

Taking the 1 mL working solution as an example, take 1 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. 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-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
in vitro	PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. ^[1]
in vivo	In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells.
	濃度	~10 μM
	反応時間	72 hours
	実験の流れ	SCLC cells are cultured (5,000 cells/well) in a 96-well microtiter plate at 37°C in 5% CO₂ in supplier-recommended growth media and compounds are added to each well starting at 10 μM with a 3-fold serial dilution. At 72 hours after compound addition, CellTiter-Glo (CTG) Solution is added per the manufacturer's instructions. Luminescence is read on an Envision plate reader. All experiments are run in duplicate and have been repeated at least three times.
動物実験	動物モデル	SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors
	投薬量	350 mg/kg
	投与方法	p.o.

参考

[1] Walls M, et al. Clin Cancer Res. 2014, 20(3), 631-643.

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：

Overexpression of ATP-Binding Cassette Subfamily G Member 2 Confers Resistance to Phosphatidylinositol 3-Kinase Inhibitor PF-4989216 in Cancer Cells. [ Mol Pharm, 2017, 14(7):2368-2377]	PubMed: 28597653

Overexpression of ATP-Binding Cassette Subfamily G Member 2 Confers Resistance to Phosphatidylinositol 3-Kinase Inhibitor PF-4989216 in Cancer Cells. [ Mol Pharm, 2017, 14(7):2368-2377]

PubMed: 28597653

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。