895158-95-9
SC144
CAS: 895158-95-9
Molecular Formula: C16H11FN6O
895158-95-9 - Names and Identifiers
895158-95-9 - Physico-chemical Properties
| Molecular Formula | C16H11FN6O |
| Molar Mass | 322.3 |
| Density | 1.53±0.1 g/cm3(Predicted) |
| pKa | 8.87±0.43(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC 50 s in a submicromolar range (IC 50 =OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM). The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC 50 =0.43 μM) and HEY (Cisplatin-resistant, IC 50 =0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells. 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. 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. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis. Apoptosis Analysis Cell Line: OVCAR-8 and Caov-3 cells Concentration: 2 μM Incubation Time: 24 hours Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells. Western Blot Analysis Cell Line: OVCAR-8, Caov-3 cells Concentration: 0.5-2 μM Incubation Time: 0-6 hours Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner. |
| In vivo study | SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts. 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. Animal Model: Athymic mice (human ovarian cancer xenograft) Dosage: 10 mg/kg Administration: I.p; daily for 58 days Result: Significantly inhibited tumor growth by about 73%. |
895158-95-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.103 ml | 15.513 ml | 31.027 ml |
| 5 mM | 0.621 ml | 3.103 ml | 6.205 ml |
| 10 mM | 0.31 ml | 1.551 ml | 3.103 ml |
| 5 mM | 0.062 ml | 0.31 ml | 0.621 ml |
Last Update：2024-01-02 23:10:35
895158-95-9 - Reference Information
| introduction | SC144 is an orally active small molecule gp130 inhibitor. |
| biological activity | SC144 is the first oral active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, eliminates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 has obvious inhibitory effect on signal transduction triggered by gp130 ligand. SC144 induces apoptosis in human ovarian cancer cells. |
| target | IL6-beta |
| in vitro study | SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC 50 s in a submicromolar range (IC 50 = OVCAR-8, OVCAR-5, OVCAR-3 = 0.72, 0.49, 0.95 μ m). The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC 50=0.43 μ m) and HEY (Cisplatin-resistant, IC 50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells. 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 banner. 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. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis. Apoptosis Analysis Cell Line: OVCAR-8 and Caov-3 cells Concentration: 2 μM Incubation Time: 24 hours Result: Significantly used cell death in OVCAR-8 and Caov-3 cells. Western Blot Analysis Cell Line: OVCAR-8, Caov-3 cells Concentration: 0.5-2 μM Incubation Time: 0-6 hours Result: substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner. |
| Cell Line: | OVCAR-8 and Caov-3 cells OVCAR-8, Caov-3 cells |
| Concentration: | 2 μM 0.5-2 μM |
| Incubation Time: | 24 hours 0-6 hours |
| Result: | Significantly causeed cell death in OVCAR-8 and Caov-3 cells. Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner. Significantly inhibited tumor growth by about 73%. |
| in vivo study | SC144 (10 mg/kg; I.p.; Daily for 58 days) suppresses tumor growth in human ovariancancer xenografts. SC144 (100 mg/kg;p.o.; Daily for 35 days) treatment show the average volume in mice 82% smaller that that in the control group. Animal Model: athymic mice (human ovarian cancer xenograft) Dosage: 10 mg/kg Administration: I.p; Daily for 58 days Result: Significantly inhibited tumor growth by about 73%. |
| Animal Model: | Athymic mice (human ovarian cancer xenograft) |
| Dosage: | 10 mg/kg |
| Administration: | I .p; daily for 58 days |
Last Update：2024-04-09 20:52:54
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Tel: 609-228-6898
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tech@medchemexpress.com
Mobile: 609-228-6898
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