SC144 hydrochloride is the first oral active GP130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, inducing phosphorylation (S782) and deglycosylation of GP130, eliminating Stat3 phosphorylation and nuclear translocation, and further inhibiting the expression of downstream target genes. SC144 hydrochloride inhibited signal transduction induced by GP130 ligand. SC144 hydrochloride induces apoptosis of human ovarian cancer cells.
| Molecular Weight | 358.76 |
| Formula | C16H11FN6O.HCl |
| CAS Number | 917497-70-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 32.23 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.
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