SC144

製品コードS7124 バッチS712402

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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.500mg/ml (1.55mM) Taking the 1 mL working solution as an example, add 50 μL of 10 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 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. This compound shows synergism when co-treated in colorectal cancer HT29 cells. In addition, the combination of this chemical exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. [1] Its 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, it 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 this 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 this compound 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 this chemical delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of this compound reveals that intraperitoneal administration of this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/19322070/
  • https://pubmed.ncbi.nlm.nih.gov/23536726/

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：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
Monocyte-derived macrophages support alveolar regeneration via oncostatin M post-H1N1 infection during the recovery phase [ Respir Res, 2025, 26(1):285] PubMed: 41063200
Glycoprotein 130 Antagonism Counteracts Metabolic and Inflammatory Alterations to Enhance Right Ventricle Function in Pulmonary Artery Banded Pigs [ bioRxiv, 2025, 2025.01.20.633954] PubMed: 39896622
Multiomic analyses uncover immunological signatures in acute and chronic coronary syndromes [ Nat Med, 2024, 30(6):1696-1710] PubMed: 38773340
Multiomic analyses uncover immunological signatures in acute and chronic coronary syndromes [ Nat Med, 2024, 10.1038/s41591-024-02953-4] PubMed: 38773340
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

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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