Name: SC144
Brand: Selleck Chemicals
SKU: S7124
Availability: InStock
Rating: 5 (19 reviews)

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Anti-infection Antioxidant COX Histamine Receptor
Other Interleukins Inhibitors	Ossirene (AS101) Diacerein Ac-YVAD-cmk Apilimod mesylate EC330 Sodium Thiocyanate IQ 3 Raleukin Cp2-SO4 Suplatast Tosylate

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (198.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.
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	30%propylene glycol 1 5%Tween80 2 65%D5W (oral gavage) Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (93.08mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W (oral gavage) to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	322.3	Formula	C₁₆H₁₁FN₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	895158-95-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4

Mechanism of Action

Targets/IC₅₀/Ki	gp130
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19322070/ [2] https://pubmed.ncbi.nlm.nih.gov/23536726/

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SC144 GP130 Inhibitor

Chemical Structure

Molecular Weight: 322.3