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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H17N3O4S |
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分子量 | 347.39 | CAS No. | 1403764-72-6 | |
Solubility (25°C)* | 体外 | DMSO | 69 mg/mL (198.62 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay. |
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in vitro | PFI-1 binds to with cyclic AMP response binding protein with KD of 49 μM. PFI-1 has an EC50 of 1.89 μM for the inhibition of IL6 production from human blood mononuclear cells stimulated by LPS. [1] PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. [2] PFI-1 inhibits the proliferating of three NET cell lines (Bon-1 derived from a pancreatic NET, and H727 and H720 derived from lung NETs). [3] |
in vivo | PFI-1 administrated (1 mg/kg i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18/mL·min–1·kg–1 and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours. [1] |
細胞アッセイ | 細胞株 | T4302 CD133+ cells |
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濃度 | 1 mM | |
反応時間 | 5 days | |
実験の流れ | To determine dose response, cells are aliquoted into 96-well plate at 5 × 103 cells per well in triplicates. PFI-1 is added by 2- or 4-fold serial dilutions. Cell number is measured 5 days after plating using the CellTiter-Glo Kit and normalized to corresponding vehicle-treated groups. IC50 values are calculated by the GraphPad Prism 5 software using the 4-parameter logistic nonlinear regression model. To calculate the relative growth of cells, averaged cell titers of each group on day 1 are assigned a value of 1. All subsequent cell titer values are normalized accordingly. |
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動物実験 | 動物モデル | Rats |
投薬量 | 1 mg/kg | |
投与方法 | Intravenous injection |
CBX5 loss drives EGFR inhibitor resistance and results in therapeutically actionable vulnerabilities in lung cancer [ Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120] | PubMed: 36652476 |
Glutathione peroxidase 8 expression on cancer cells and cancer-associated fibroblasts facilitates lung cancer metastasis [ MedComm (2020), 2022, 3(3):e152] | PubMed: 35978854 |
Bromodomain-containing protein 4 (BRD4) as an epigenetic regulator of fatty acid metabolism genes and ferroptosis [ Cell Death Dis, 2022, 13(10):912] | PubMed: 36309482 |
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] | PubMed: 35758684 |
A PGE2-MEF2A axis enables context-dependent control of inflammatory gene expression [ Immunity, 2021, S1074-7613(21)00222-3] | PubMed: 34129840 |
Isoform-specific Involvement of Brpf1 in Expansion of Adult Hematopoietic Stem and Progenitor Cells [ J Mol Cell Biol, 2020, 11;12(5):359-371] | PubMed: 31565729 |
IRF1 Maintains Optimal Constitutive Expression of Antiviral Genes and Regulates the Early Antiviral Response. [ Front Immunol, 2019, 1.1243055556] | PubMed: 31156620 |
The BET-inhibitor PFI-1 diminishes AR/AR-V7 signaling in prostate cancer cells. [ World J Urol, 2019, 37(2):343-349] | PubMed: 29934670 |
A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer. [ Nat Commun, 2017, 8:14802] | PubMed: 28378740 |
BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency. [ Sci Rep, 2017, 7(1):16646] | PubMed: 29192216 |
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。