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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 | |
|---|---|
| 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, as described previously (Ple´ et al., 2004). Briefly, cells were plated onto 96-well plates (1.5*10^4 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 | |
|---|---|
| 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 |
| Related Src-bcr-Abl Products |
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Ponatinib (AP24534) is a novel potent, orally available small molecule multitargeted kinase inhibitor of BCR-ABL, PDGFRα, c-Src, c-Kit, FGFR and VEGFR. |
| Bosutinib
Bosutinib (SKI-606) is a novel Bcr-Abl inhibitor with IC50 values of 0.1 to 0.3 umol/L. |
| Dasatinib
Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. |
| DCC-2036
DCC-2036 is an ABL inhibitor with IC50 of 0.8 and 2 nM for u-ABL1native and p-ABL1native, respectively. |
| Imatinib Mesylate
Imatinib Mesylate is a Bcr-Abl tyrosine kinase inhibitor, with IC50 values of 2.9 and 3.9 μM for the inhibition of T-cell proliferation stimulated by PHA and DCs respectively. |
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