FLLL32

製品コードS7259 バッチS725901

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

C28H32O6

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)
Clear solution
5% DMSO 95% Corn oil
0.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ JAK2 and other human kinase activity assays
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.

カスタマーフィードバック

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]

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:

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。

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