SC144

製品コードS7124 バッチS712403

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

C16H11FN6O
分子量 322.3 CAS No. 895158-95-9
Solubility (25°C)* 体外 DMSO 64 mg/mL (198.57 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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES
濃度 ~10 μM
反応時間 96 h
実験の流れ

MTT assay
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.

カスタマーフィードバック

Data from [Data independently produced by , , Cell Death Dis, 2016, 7(8):e2339.]

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：

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。

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