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Purity: ≥98%
SC144 is a first-in-class small-molecule inhibitor of gp130 with oral activity in ovarian cancer. It can substantially increase the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner. The increase phosphorylation then suppresses Stat3 signaling pathway since the constitutive Stat3 activation is maintained by extracellular gp130 ligands, Besides that, SC144 also causes substantial cell apoptosis in these cells.
| ln Vitro |
In a panel of human ovarian cancer cell lines, SC144 inhibits cell proliferation with IC50s in the submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1]. SC144's potency against NCI/ADR-RES (a resistance to Paclitaxel and Doxorubicin; IC50=0.43 μM) and HEY (a resistance to Cisplatin; IC50=0.88 μM) indicates that it may be able to overcome medication resistance in ovarian cancer[1]. Normal kidney epithelium and normal endometrial cells do not produce as much apoptosis in OVCAR-8 and Caov-3 as does SC144 (2 μM; 24 hours)[1]. In a time- and dose-dependent way, SC144 (0.5-2 μM; 0–6 hours) significantly increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells[1]. Through the regulation of Stat3-regulated gene expression and the inactivation of Akt and Stat3, SC144 is cytotoxic to ovarian cancer cells through the inhibition of gp130 function. Consequently, SC144 therapy ultimately results in apoptosis, anti-angiogenesis, and cell-cycle arrest[1].
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| ln Vivo |
In human ovarian cancer xenografts, SC144 (10 mg/kg; ip; daily for 58 days) inhibits the growth of tumors[1]. ?The average tumor volume in mice treated with SC144 (100 mg/kg; po; daily for 35 days) was 82% lower than in the control group[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: OVCAR-8 and Caov-3 cells Tested Concentrations: 2 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically caused cell death in OVCAR-8 and Caov-3 cells. Western Blot Analysis[1] Cell Types: OVCAR-8, Caov-3 cells Tested Concentrations: 0.5-2 μM Incubation Duration: 0-6 hrs (hours) Experimental Results: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Athymic mice (human ovarian cancer xenograft)[1]
Doses: 10 mg/kg Route of Administration: Ip; daily for 58 days Experimental Results: Dramatically inhibited tumor growth by about 73%. |
| References |
[1]. Xu S, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.
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| Molecular Formula |
C16H11FN6O
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| Molecular Weight |
322.3
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| CAS # |
895158-95-9
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| Related CAS # |
SC144 hydrochloride;917497-70-2
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| SMILES |
O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3
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| Chemical Name |
2-Pyrazinecarboxylic Acid 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
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| Synonyms |
SC-144; SC144; SC 144;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1027 mL | 15.5135 mL | 31.0270 mL | |
| 5 mM | 0.6205 mL | 3.1027 mL | 6.2054 mL | |
| 10 mM | 0.3103 mL | 1.5513 mL | 3.1027 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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