Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.Saracatinib (AZD0530) demonstrated potent antimigratory and antiinvasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. Antiproliferative activity of AZD0530 in vitro varied between cell lines (IC50=0.2 ~10 mM).
Cell Experiment | |
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Cell lines | Calu-6, A549, LoVo, SW 403, HT29, HCT 116 and other cells line |
Preparation method | Cell proliferation was assessed using a colorimetric 5-bromo- 20 -deoxyuridine (BrdU) Cell Proliferation ELISA kit (Roche Diagnostics GmbH), as described previously (Ple´ et al., 2004). Briefly, cells were plated onto 96-well plates (1.5*104 cells/ well), the following day 0.039–20 μM AZD0530 in DMSO (at a final concentration of 0.5%) was added and the cells were incubated for 24 h. The cells were pulse labeled with BrdU for 2 h and fixed. Cellular DNA was then denatured with the provided solution and incubated with antiBrdU peroxidase for 90 min. Following three washes with phosphate-buffered saline, tetramethylbenzidine substrate solution was added and the plates were incubated on a plate shaker for 10–30 min until the positive control absorbance at 690 nm was approximately 1.5 absorbance units. |
Concentrations | 0.039–20 μM |
Incubation time | 24 h |
Animal Experiment | |
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Animal models | female nude mice bearing LoVo tumors, Src3T3 allografts and human NSCLC (Calu-6) xenografts |
Formulation | saline |
Dosages | 6.25–50 mg/kg for 10–91 days |
Administration | oral gavage |
Molecular Weight | 542.03 |
Formula | C27H32ClN5O5 |
CAS Number | 379231-04-6 |
Solubility (25°C) | DMSO 33 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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