PFK15

카탈로그 번호S7289 배치:S728901

인쇄

기술 자료

화학식

C17 H12 N2 O
분자량 260.29 CAS 번호 4382-63-2
용해도 (25°C)* 시험관 내(In vitro) DMSO 19 mg/mL (72.99 mM)
Ethanol 2 mg/mL (7.68 mM)
Water Insoluble
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
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/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 PFK15 (PFK-015) 6-phosphofructo-2-kinase (PFKFB3) 207 nM IC50 .
표적
PFKFB3
(Cell-free assay)
207 nM
시험관 내(In vitro) PFK15 Jurkat T H522 F26BP, ATP .
생체 내(In Vivo) In vivo, PFK15 . (25 mg/kg i.p.) syngeneic LLC , , . athymic xenograft .

프로토콜 (참조)

키나아제 분석:

[1]
  • PFKFB3

    13 ng PFKFB3 10 /L ATP, 10 /L F6P, DMSO ( ) , 3PO, PFK15 1 . Adapta Universal Kinase Assay .
세포 분석:

[1]
  • 세포주

    59 cancer cell lines

  • 농도

    ~30 μM

  • 배양 시간

    48 hours

  • 방법

    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.
동물 연구:

[1]
  • 동물 모델

    C57Bl/6 mice bearing LLC xenografts, Balb/C athymic mice bearing CT26, U-87 MG, or BxPC-3 xenografts.

  • 용량

    25 mg/kg every 3 days

  • 투여

    i.p.

참조

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

고객 제품 검증

<p>b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays.</p>

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

RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone

데이터 출처 [ , , Br J Pharmacol, 2017, 174(9):893-908 ]

(a, b) Cells were treated with the indicated concentrations of PFK15 for 12 h in the upper chambers and the lower chambers were filled with 10% FBS medium. Then, the invaded cells were stained with crystal violet and observed under a microscope with 200× magnification. Data were obtained from six randomly chosen fields and were normalized to the control group. (c) Proteins related with cell migration and invasion were detected. Phospho-FAK levels were downregulated in 7 and 9 μM while phospho-Cadherin E levels upregulated in both cell lines. Columns, mean; bars, SD. *P<0.05, compared with controls.

데이터 출처 [ , , PLoS One, 2016, 11(9):e0163768 ]

Sellecks PFK15 인용됨 30 출판물

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
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

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