Home Transmembrane Transporters P-gp inhibitor SC144 For research use only.

SC144

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.

SC144 Chemical Structure

SC144 Chemical Structure

CAS: 895158-95-9

Selleck's SC144 has been cited by 14 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.88%
99.88

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Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCap cells Cytotoxicity assay 72 h Cytotoxicity against human LNCap cells after 72 hrs by MTT assay, IC50=0.4 μM 17085054
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells expressing p53 gene after 72 hrs by MTT assay, IC50=0.6 μM 17085054
HT29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT29 cells after 72 hrs by MTT assay, IC50=0.9 μM 17085054
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by MTT assay, IC50=0.9 μM 17085054
MDA-MB-435 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=4 μM 17085054
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Targets
gp130 [1]
In vitro
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]
Cell Research Cell lines OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES
Concentrations ~10 μM
Incubation Time 96 h
Method

MTT assay
In Vivo
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]
Animal Research Animal Models Human Ovarian Cancer OVCAR-8 Xenograft
Dosages 10 mg/kg daily
Administration i.p. or p.o.

Chemical Information & Solubility

Molecular Weight 322.3 Formula

C16H11FN6O
CAS No. 895158-95-9 SDF Download SC144 SDF
Smiles C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (198.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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