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 downstream target gene expression. SC144 inhibited signal transduction induced by GP130 ligand. SC144 induces apoptosis of human ovarian cancer cells.
| Cell Experiment | |
|---|---|
| Cell lines | OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES |
| Preparation method | MTT assay |
| Concentrations | ~10 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Human Ovarian Cancer OVCAR-8 Xenograft |
| Formulation | .9% NaCl with 40% propylene glycol |
| Dosages | 10 mg/kg daily |
| Administration | i.p. or p.o. |
| Molecular Weight | 322.3 |
| Formula | C16H11FN6O |
| CAS Number | 895158-95-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Takashi Oshima, et al. Combination effects of SC144 and cytotoxic anticancer agents
| Related IL Receptor/Related Products |
|---|
| Ebdarokimab
Ebdarokimab is a monoclonal antibody to IL-12p40/IL-23 that can be used in studies related to inflammatory bowel disease (IBD). |
| Brazikumab
Brazikumab is a human IgG2 monoclonal antibody targeting IL-23 that selectively binds to the p19 subunit of IL-23 and has a KD value of 0.138 nM against human IL-23 for Crohn's disease (CD). |
| DC-806
DC-806 is an orally active small molecule inhibitor of IL-17 for studies related to psoriasis. |
| JNJ-2113
JNJ-2113 is a novel, orally active IL-23R peptide inhibitor for studies related to plaque psoriasis. |
| PF-04236921
PF-04236921 is a fully human IgG2 monoclonal antibody targeting the interleukin IL-6 for studies related to Crohn's disease and rheumatoid arthritis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
