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AZ628 is a potent tyrosine protein inhibitor for wild-type CRAF and BRAF V600E with IC50 of 29 and 34 nM, respectively. AZ628 inhibits activities of preactivated wild-type B-Raf with an IC50 of 105, respectively. AZ628 also suppreses activities of a number of tyrosine protein kinases such as VEGFR2, DDR2, Lyn and Flt1. AZ628 also prevents anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and triggers apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. AZ628 is antiangiogenic based on inhibition of VEGFR2.
Oncogene. 2021 Jun;40(24):4137-4150.
Targeting the p300/NONO axis sensitizes melanoma cells to BRAF inhibitors
AZ628 purchased from AbMole
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Source | Cancer Discov (2013). Figure 5. AZ628 |
| Method | Western blotting | |
| Cell Lines | A375 cells | |
| Concentrations | 0.2 μM | |
| Incubation Time | 16 h | |
| Results | In contrast to the aforementioned drug conditions, only minimal resistance (2-fold) was observed to AZ628 |
| Cell Experiment | |
|---|---|
| Cell lines | The human melanoma cell |
| Preparation method | Cells were maintained at 37°C in a humidified atmposphere at 5% CO2 grown in RPMI 1640 supplemented with 10% FBS, 100 IU/mL penicillin, 100 μg/mL streptomycin and 2nM glutamine. AZ628 resistant M14 clones were maintained in the above-mentioned medium and 2 μM of AZ628, except where otherwise indicated. The BRAF inhibitor AZ628 was synthesized by Astra Zeneca. |
| Concentrations | 2 μM |
| Incubation time | 16 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 451.52 |
| Formula | C27H25N5O2 |
| CAS Number | 878739-06-1 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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