PFK15

製品コードS7289 バッチS728903

印刷

化学情報

Chemical Structure Synonyms PFK-015 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17 H12 N2 O
分子量 260.29 CAS No. 4382-63-2
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 52 mg/mL (199.77 mM)
Ethanol (warmed with 50ºC water bath) 20 mg/mL (76.83 mM)
Water Insoluble
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 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
5% DMSO 95% Corn oil
1.25mg/ml
* <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 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
in vitro PFK15 produces potent growth inhibition in a series of cancer cells. In Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells, PFK15 also reduces F26BP, glucose uptake, and intracellular ATP level. [1]
in vivo In vivo, PFK15 has adequate pharmacokinetic properties. PFK15 (25 mg/kg i.p.) suppresses the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three human xenograft models of cancer in athymic mice, PFK15 also yields antitumor effects that are comparable to approved chemotherapeutic agents. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Recombinant PFKFB3 assay
Kinase reactions are conducted by incubating 13 ng of recombinant human PFKFB3 protein in a reaction mix containing 10 μmol/L ATP, 10 μmol/L F6P, and either dimethyl sulfoxide (DMSO) vehicle control, 3PO, or PFK15 for 1 hour at room temperature. Kinase activity is measured with the Adapta Universal Kinase Assay per manufacturer
細胞アッセイ 細胞株 59 cancer cell lines
濃度 ~30 μM
反応時間 48 hours
実験の流れ

Viability is determined using trypan blue exclusion. Cells were incubated in 20% trypan blue for 5 minutes. Cells excluding trypan blue are counted using a standard hemocytometer to determine the total number of viable cells. Experiments are conducted in triplicate.
動物実験 動物モデル C57Bl/6 mice bearing LLC xenografts, Balb/C athymic mice bearing CT26, U-87 MG, or BxPC-3 xenografts.
投薬量 25 mg/kg every 3 days
投与方法 i.p.

カスタマーフィードバック

, , J Exp Clin Cancer Res, 2017, 36(1):7

Data from [Data independently produced by , , Br J Pharmacol, 2017, 174(9):893-908]

Data from [Data independently produced by , , PLoS One, 2016, 11(9):e0163768]

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：

Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] PubMed: 37689702
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
PFKFB3-mediated Pro-glycolytic Shift in Hepatocellular Carcinoma Proliferation [ Cell Mol Gastroenterol Hepatol, 2023, 15(1):61-75] PubMed: 36162723
Long noncoding RNA LINC00930 promotes PFKFB3-mediated tumor glycolysis and cell proliferation in nasopharyngeal carcinoma [ J Exp Clin Cancer Res, 2022, 41(1):77] PubMed: 35209949
CYLD deficiency enhances metabolic reprogramming and tumor progression in nasopharyngeal carcinoma via PFKFB3 [ Cancer Lett, 2022, S0304-3835(22)00055-6] PubMed: 35131382
Metabolic reprogramming by dual-targeting biomimetic nanoparticles for enhanced tumor chemo-immunotherapy [ Acta Biomater, 2022, 148:181-193] PubMed: 35649505
PFKFB3 mediates tubular cell death in cisplatin nephrotoxicity by activating CDK4 [ Transl Res, 2022, S1931-5244(22)00220-1] PubMed: 36243313
Increased stromal PFKFB3-mediated glycolysis in inflammatory bowel disease contributes to intestinal inflammation [ Front Immunol, 2022, 13:966067] PubMed: 36405760
Glucose metabolism inhibitor PFK-015 combined with immune checkpoint inhibitor is an effective treatment regimen in cancer [ Oncoimmunology, 2022, 11(1):2079182] PubMed: 35707221

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。