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SC144

Catalog No. T6207   CAS 895158-95-9

SC144 is an orally active small-molecule gp130 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SC144 Chemical Structure
SC144, CAS 895158-95-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 68.00
25 mg In stock $ 139.00
50 mg In stock $ 233.00
100 mg In stock $ 392.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 99.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SC144 is an orally active small-molecule gp130 inhibitor.
Targets&IC50 Gp130:< 1 μM (Cell assay)
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]
Cell Research MTT assay (Only for Reference)
Molecular Weight 322.3
Formula C16H11FN6O
CAS No. 895158-95-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 27 mg/mL (83.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Oshima T, et al. Anticancer Drugs, 2009, 20(5), 312-320. 2. Xu S, et al. Mol Cancer Ther, 2013, 12(6), 937-949.

TargetMolCitations

1. Guo C, Dong J, Ma Y, et al. LIF and bFGF enhanced chicken primordial follicle activation by Wnt/β-catenin pathway. Theriogenology. 2021

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Immunology/Inflammation Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Apoptosis Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library Anti-Ovarian Cancer Compound Library Orally Active Compound Library

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Keywords

SC144 895158-95-9 Apoptosis Immunology/Inflammation Interleukin SC-144 anti-angiogenesis Inhibitor oral inhibit SC 144 arrest translocation ovarian nuclear Interleukin Related phosphorylation cancer cell-cycle inhibitor

 

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