SC144

카탈로그 번호S7124 배치:S712401

인쇄

기술 자료

화학식

C16H11FN6O
분자량 322.3 CAS 번호 895158-95-9
용해도 (25°C)* 시험관 내(In vitro) DMSO 28 mg/mL (86.87 mM)
Water Insoluble
Ethanol Insoluble
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
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.
* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 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.
표적
gp130
시험관 내(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.

생체 내(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.

프로토콜 (참조)

세포 분석:

[2]
  • 세포주

    OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES

  • 농도

    ~10 μM

  • 배양 시간

    96 h

  • 방법

    MTT assay
동물 연구:

[2]
  • 동물 모델

    Human Ovarian Cancer OVCAR-8 Xenograft

  • 용량

    10 mg/kg daily

  • 투여

    i.p. or p.o.

참조

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

고객 제품 검증

Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.

데이터 출처 [ , , Cell Death Dis, 2016, 7(8):e2339. ]

Selleck's SC144 인용됨 24 출판물

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

반품 정책
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배송 및 보관
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