TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), with IC50 values between 13.9 and 51.1 μM against several human cancer cell lines. TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441 increases apoptosis in HT1080 and HCT116 cells.
In vivo, TM5441 (20 mg/kg/day; Oral) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival.
| Molecular Weight | 428.82 |
| Formula | C21H17ClN2O6 |
| CAS Number | 1190221-43-2 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 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.
| Related PAI-1 Products |
|---|
| Glutaryl-Gly-Arg-AMC
Glutaryl-Gly-Arg-AMC is a peptide substrate of urokinase plasminogen activator (uPA). |
| GGACK
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor. |
| PPACK
PPACK is a plasminogen activator (rt-PA) inhibitor. |
| Anecortave acetate
Anecortave acetate is a potent ocular vascular inhibitor that inhibits angiogenic factor-induced neointima formation and also increases fibrinogen activator inhibitor 1 (PAI-1) mRNA expression.Anecortave acetate can be used in studies related to ocular neovascularization diseases. |
| SK-216
SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma. |
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