SC144

製品コードS7124 バッチS712403

化学情報

	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は、gp130のリン酸化（S782）と脱グリコシル化を誘導し、Stat3のリン酸化と核内移行を阻害し、さらに下流の標的遺伝子の発現を抑制する、ファーストインクラスの経口活性小分子gp130阻害剤です。
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. 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.
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. 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.

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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