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 |
| 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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