LY2874455

製品コードS7057 バッチS705703

印刷

化学情報

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

C21H19Cl2N5O2
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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ Biochemical filter-binding assays for detection of FGFR phosphorylation activities
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).
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.

カスタマーフィードバック

Data from [Data independently produced by , , PLoS One. 2016, 11(9): e0162491]

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：

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。

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