TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors, with IC50 values of 30 and 32 nM for rVEGFR2 and rMET, respectively.
In vivo, TAS-115 (Pamufetinib) completely suppressed the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 (Pamufetinib) induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity.
| Cell Experiment | |
|---|---|
| Cell lines | PC-9 (del E746_A750) and HCC827 |
| Preparation method | Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 μM) or erlotinib (0.3 μM) in the lower Transwell collagen–coated chambers are cocultured with MRC-5 (1000 cells/300 μL) cells in the upper chamber for 72 hours. The upper chamber is then removed. Cell viability is measured using the MTT assay. |
| Concentrations | 1.0 μmol/liter |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | SC-9 tumor-bearing nude mice |
| Formulation | - |
| Dosages | 12.5, 50, and 200 mg/kg/d |
| Administration | orally |
| Molecular Weight | 614.66 |
| Formula | C28H27FN4O7S2 |
| CAS Number | 1688673-09-7 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage | 2-8°C, dry, sealed |
| 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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| KLTWQELYQLKYKGI
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| Protein LMWP
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| CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
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