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SC144 is an orally active small-molecule gp130 inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $39 | In Stock | In Stock | |
| 10 mg | $68 | In Stock | In Stock | |
| 25 mg | $139 | In Stock | In Stock | |
| 50 mg | $233 | In Stock | In Stock | |
| 100 mg | $392 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock | In Stock |
| 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 |
| Smiles | Cl.Fc1ccc2c(c1)nc(NNC(=O)c1cnccn1)c1cccn21 |
| Relative Density. | 1.53 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 15 mg/mL (46.54 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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