受注:045-509-1970 |
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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 | C21H19Cl2N5O2 |
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分子量 | 444.31 | CAS No. | 1254473-64-7 | |
Solubility (25°C)* | 体外 | DMSO | 88 mg/mL (198.05 mM) | |
Ethanol | 88 mg/mL warmed with 50ºC water bath (198.05 mM) | |||
Water | 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 | LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1. |
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in vitro | In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and KATO-III cells. [1] |
in vivo | LY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth. [1] |
キナーゼアッセイ | Biochemical filter-binding assays for detection of FGFR phosphorylation activities | |
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Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader. | ||
細胞アッセイ | 細胞株 | KMS-11, OPM-2, L-363, U266, SNU-16, KATO-III, NUGC-3 and SH-10-TC cells |
濃度 | ~1 μM | |
反応時間 | 72 hours | |
実験の流れ | Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). |
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動物実験 | 動物モデル | Mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft |
投薬量 | 3 mg/kg | |
投与方法 | p.o. |
Data from [Data independently produced by , , PLoS One. 2016, 11(9): e0162491]
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] | PubMed: 37377403 |
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] | PubMed: 37377403 |
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] | PubMed: 37377403 |
Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] | PubMed: 35732112 |
Strategies to inhibit FGFR4 V550L-driven rhabdomyosarcoma [ Br J Cancer, 2022, 10.1038/s41416-022-01973-6] | PubMed: 36097178 |
Targeting PEA3 transcription factors to mitigate small cell lung cancer progression [ Oncogene, 2022, 10.1038/s41388-022-02558-6] | PubMed: 36509998 |
Sensitization of osteosarcoma to irradiation by targeting nuclear FGFR1 [ Biochem Biophys Res Commun, 2022, 621:101-108] | PubMed: 35820279 |
The cytokine FAM3B/PANDER is an FGFR ligand that promotes posterior development in Xenopus [ Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118] | PubMed: 33975953 |
Depletion of CLK2 sensitizes glioma stem-like cells to PI3K/mTOR and FGFR inhibitors [ Am J Cancer Res, 2020, 10(11):3765-3783] | PubMed: 33294266 |
Chemical genomics reveals inhibition of breast cancer lung metastasis by Ponatinib via c-Jun. [ Protein Cell, 2019, 10(3):161-177] | PubMed: 29667003 |
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。