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A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation.The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher compound accumulation of F-SL in the tumor than liposome alone at 24 h post injection.
*The compound is unstable in solutions, freshly prepared is recommended
 |
Application | MTT assay |
| Results | As shown in Fig. 6c that A83-01 alone reduced approximately 17% cell migration of JIMT1 and trastuzumab alone inhibited 20% cell migration, while in combination of A83-01 and trastuzumab synergistically inhibited JIMT1 cell migration up to 90%. |
| Cell Experiment | |
|---|---|
| Cell lines | HM-1 cells |
| Preparation method | HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay. |
| Concentrations | 1 μM |
| Incubation time | 12 hr |
| Animal Experiment | |
|---|---|
| Animal models | Female B6C3F1 mice injected with HM-1 cells (1×10^6) |
| Formulation | PBS with 0.5% DMSO |
| Dosages | 150 μg/body, three times per week |
| Administration | injected into the abdominal cavity |
| Molecular Weight | 421.52 |
| Formula | C25H19N5S |
| CAS Number | 909910-43-6 |
| Solubility (25°C) | DMSO 24 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
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