PFK15

製品コードS7289 バッチS728901

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) 19 mg/mL (72.99 mM)
Ethanol (warmed with 50ºC water bath) 2 mg/mL (7.68 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
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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, this compound also reduces F26BP, glucose uptake, and intracellular ATP level. [1]
in vivo In vivo, PFK15 has adequate pharmacokinetic properties. This compound (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, it 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23674815/

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：

Transient APC/C inactivation by mTOR boosts glycolysis during cell cycle entry [ Nature, 2025, 10.1038/s41586-025-09328-w] PubMed: 40739344
Immunosuppressive Formulations for Immunological Defense against Traumatic Brain Injury [ Adv Healthc Mater, 2025, e2501417.] PubMed: 40437894
Vitamin D impedes eosinophil chemotaxis via inhibiting glycolysis-induced CCL26 expression in eosinophilic chronic rhinosinusitis with nasal polyps [ Cell Commun Signal, 2025, 23(1):104] PubMed: 39985085
Live-cell metabolic analyzer protocol for measuring glucose and lactate metabolic changes in human cells [ STAR Protoc, 2025, 6(1):103518] PubMed: 39799573
Identification of PFKFB3 as a key factor in the development of colorectal cancer and immunotherapy resistance [ Clin Exp Med, 2024, 24(1):219] PubMed: 39261380
Multi-omics and immunogenomics analysis revealed PFKFB3 as a targetable hallmark and mediates sunitinib resistance in papillary renal cell carcinoma: in silico study with laboratory verification [ Eur J Med Res, 2024, 29(1):236] PubMed: 38622715
Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] PubMed: 37689702
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

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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