SC144 hydrochloride (HCl) is a first-in-class, powerful, and orally bioavailable small-molecule gp130 inhibitor that inhibits cell growth in a panel of human ovarian cancer cell lines with an IC50 in the submicromolar range.
Physicochemical Properties
| Molecular Formula | C₁₆H₁₂CLFN₆O |
| Molecular Weight | 358.76 |
| Exact Mass | 358.075 |
| Elemental Analysis | C, 53.57; H, 3.37; Cl, 9.88; F, 5.30; N, 23.43; O, 4.46 |
| CAS # | 917497-70-2 |
| Related CAS # | SC144;895158-95-9 |
| PubChem CID | 66921431 |
| Appearance | Light yellow to gray solid powder |
| Melting Point | 282 °C (decomp) (methanol) |
| LogP | 3.439 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 3 |
| Heavy Atom Count | 25 |
| Complexity | 466 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | Cl.O=C(C1C=NC=CN=1)NNC1C2N(C=CC=2)C2C(=CC(=CC=2)F)N=1 |
| InChi Key | LKFGGXYXFIICED-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C16H11FN6O.ClH/c17-10-3-4-13-11(8-10)20-15(14-2-1-7-23(13)14)21-22-16(24)12-9-18-5-6-19-12;/h1-9H,(H,20,21)(H,22,24);1H |
| Chemical Name | N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide;hydrochloride |
| Synonyms | SC-144; SC144; SC 144 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | IL6-beta |
| ln Vitro |
SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1]. The effectiveness of SC144 against NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 M) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1]. OVCAR-8 and Caov-3 experience a significant increase in apoptosis when exposed to SC144 (2 μM; 24 hours) compared to normal kidney epithelial and normal endometrial cells[1]. SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1]. SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. Cell-cycle arrest, anti-angiogenesis, and apoptosis are consequent effects of SC144 treatment[1]. |
| ln Vivo | SC144 (10 mg/kg; i.p.; daily for 58 days) inhibits the development of tumors in human ovarian cancer xenografts[1]. SC144 (100 mg/kg; p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1]. |
| References |
[1]. 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. |
Solubility Data
| Solubility (In Vitro) |
DMSO: ~10 mg/mL (~27.9 mM) H2O: <0.1 mg/mL |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7874 mL | 13.9369 mL | 27.8738 mL | |
| 5 mM | 0.5575 mL | 2.7874 mL | 5.5748 mL | |
| 10 mM | 0.2787 mL | 1.3937 mL | 2.7874 mL |