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 | C16H11FN6O |
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分子量 | 322.3 | CAS No. | 895158-95-9 | |
Solubility (25°C)* | 体外 | DMSO | 28 mg/mL (86.87 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 | SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. |
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in vitro | SC144 exhibits potent cytotoxicity against a panel of drug-sensitive and drug-resistant cancer cell lines. SC144 shows synergism with both 5-fluorouracil and oxaliplatin when co-treated in colorectal cancer HT29 cells. Pretreatment with SC144 in oxaliplatin-resistant HTOXAR3 cells is more effective than oxaliplatin pretreatment. In addition, the combination of SC144 and paclitaxel exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. [1] SC144 treatment in vitro induces gp130 phosphorylation and deglycosylation, resulting in the downregulation of surface-bound gp130 and the abrogation of gp130-associated Stat3 activation. In addition, SC144 selectively inhibits the downstream signaling activation induced by gp130 substrates, including IL-6 and LIF. Protein expression regulated by the gp130/Stat3 axis in OVCAR-8 cells is also down-regulated after SC144 treatment, including Bcl-2, Bcl-XL, survivin, cyclin D1, MMP-7, gp130 and Ape1/Rel-1. [2] |
in vivo | SC144 significantly inhibits tumor growth in a mouse xenograft model of human ovarian cancer via i.p. or p.o. administration. After SC144 treatment for two months, gp130, Bcl-2, Bcl-XL, MMP-7 and Ape1/Ref-1 protein levels are substantially decreased in the tumor site in the treatment group compared with the control group. [2] In an MDA-MB-435 mouse xenograft model, co-administration of SC144 and paclitaxel delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of SC144 reveals that intraperitoneal administration of SC144 shows a two-compartmental pharmacokinetics elimination profile that is not observed in the oral dosing. [1] |
細胞アッセイ | 細胞株 | OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES |
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濃度 | ~10 μM | |
反応時間 | 96 h | |
実験の流れ | MTT assay |
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動物実験 | 動物モデル | Human Ovarian Cancer OVCAR-8 Xenograft |
投薬量 | 10 mg/kg daily | |
投与方法 | i.p. or p.o. |
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Data from [Data independently produced by , , Cell Death Dis, 2016, 7(8):e2339.]
Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041] | PubMed: 38310113 |
LIF signaling regulates outer radial glial to interneuron fate during human cortical development [ Cell Stem Cell, 2023, 30(10):1382-1391.e5] | PubMed: 37673072 |
Targeting the gp130/STAT3 Axis Attenuates Tumor Microenvironment Mediated Chemoresistance in Group 3 Medulloblastoma Cells [ Cells, 2022, 11(3)381] | PubMed: 35159191 |
Gp130-Mediated STAT3 Activation Contributes to the Aggressiveness of Pancreatic Cancer through H19 Long Non-Coding RNA Expression [ Cancers (Basel), 2022, 14(9)2055] | PubMed: 35565185 |
MBL Binding with AhR Controls Th17 Immunity in Silicosis-Associated Lung Inflammation and Fibrosis [ J Inflamm Res, 2022, 15:4315-4329] | PubMed: 35923908 |
Falcarindiol Enhances Cisplatin Chemosensitivity of Hepatocellular Carcinoma via Down-Regulating the STAT3-Modulated PTTG1 Pathway [ Front Pharmacol, 2021, 12:656697] | PubMed: 34025420 |
Omega‑3 polyunsaturated fatty acids inhibit IL‑11/STAT3 signaling in hepatocytes during acetaminophen hepatotoxicity [ Int J Mol Med, 2021, 48(4)190] | PubMed: 34414450 |
Inflammatory signals induce MUC16 expression in ovarian cancer cells via NF-κB activation [ Exp Ther Med, 2021, 21(2):163] | PubMed: 33456530 |
Autocrine and paracrine signaling contributes to acquired chemotherapeutic resistance in Group 3 medulloblastoma [ B.S., The University of Arizona, 2021, ] | PubMed: none |
Inhibition of STAT3 activation mediated by toll-like receptor 4 attenuates angiotensin II-induced renal fibrosis and dysfunction [ Br J Pharmacol, 2019, 176(14):2627-2641] | PubMed: 30958891 |
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。