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 | C28H32O6 |
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分子量 | 464.55 | CAS No. | 1226895-15-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 92 mg/mL (198.04 mM) | ||||||||
Ethanol (warmed with 50ºC water bath) | 25 mg/mL (53.81 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells. |
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in vitro | In MDA-MB-231 breast and PANC-1 pancreatic cancer cells, FLLL32 downregulates STAT3 phosphorylation and DNA-binding activity. In MDA-MB-231 cells, FLLL32 inhibit the formation of colonies and cell invasion. [1] In human multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cell lines, FLLL32 also leads to the inhibition of cell proliferation and the induction of caspase-3 and PARP cleavages. [2] |
in vivo | In MDA-MB-231 xenografted mice, FLLL32 (50 mg/kg, i.p.) significantly reduces tumor burdens. [1] In mouse xenografts with OS-33 osteosarcoma cells, FLLL32 (50 mg/kg, i.p.) also inhibits tumor growth by targeting STAT3. [3] |
キナーゼアッセイ | JAK2 and other human kinase activity assays | |
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JAK2 kinase activity was assessed with the HTScan JAK2 Kinase Assay Kit per manufacturer's protocol. The possible effects of FLLL32 on the other 10 purified human protein kinases were determined by using a Kinase Profiler Assay. | ||
細胞アッセイ | 細胞株 | MDA-MB-231 cell line |
濃度 | ~5 μM | |
反応時間 | 72 hours | |
実験の流れ | Cells are seeded in 96-well plates (3,000 per well) in triplicate and then treated with 0.5 to 5 μM of FLLL31 or FLLL32 or with 0.5 to 30 μM of curcumin for 72 h. MTT (25 μL) is added to each sample and incubated for 3.5 h. Then, 100 μL of N,N-dimethylformamide solubilization solution are added to each well. The absorbance at 450 nm is read the following day. IC50 are determined using Sigma Plot 9.0 software. | |
動物実験 | 動物モデル | MDA-MB-231 xenografted mice |
投薬量 | 50 mg/kg, daily | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Cancer Sci, 2016, 107(7):944-54. ]
Data from [Data independently produced by , , Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011]
JARID2 coordinates with the NuRD complex to facilitate breast tumorigenesis through response to adipocyte-derived leptin [ Cancer Commun -Lond), 2023, 43(10):1117-1142] | PubMed: 37658635 |
Melatonin attenuates chronic intermittent hypoxia-induced intestinal barrier dysfunction in mice [ Microbiol Res, 2023, 276:127480] | PubMed: 37659335 |
RING-Finger Protein 6 promotes Drug Resistance in Retinoblastoma via JAK2/STAT3 Signaling Pathway [ Pathol Oncol Res, 2022, 28:1610273] | PubMed: 35369571 |
Regulation of STUB1 expression and its biological significance in mouse Sertoli cells [ Syst Biol Reprod Med, 2022, 1-15] | PubMed: 35343345 |
Protective and anti-inflammatory role of REG1A in inflammatory bowel disease induced by JAK/STAT3 signaling axis [ Int Immunopharmacol, 2021, 92:107304] | PubMed: 33513463 |
Aberrant SLC6A14 Expression Promotes Proliferation and Metastasis of Colorectal Cancer via Enhancing the JAK2/STAT3 Pathway [ Onco Targets Ther, 2021, 14:379-392] | PubMed: 33469314 |
Tumor-associated neutrophils suppress antitumor immunity of NK cells through the PD-L1/PD-1 axis [ Transl Oncol, 2020, 13(10):100825] | PubMed: 32698059 |
B7-H3 Regulates Glioma Growth and Cell Invasion Through a JAK2/STAT3/Slug-Dependent Signaling Pathway. [ Onco Targets Ther, 2020, 12;13:2215-2224] | PubMed: 32210587 |
Downregulation of DPF3 promotes the proliferation and motility of breast cancer cells through activating JAK2/STAT3 signaling. [ Biochem Biophys Res Commun, 2019, 514(3):639-644] | PubMed: 31076105 |
SOCS3 overexpression enhances ADM resistance in bladder cancer T24 cells. [Li MZ, et al. Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011] | PubMed: 28742207 |
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。