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AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM.AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.
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Source | Eur J Cancer (2013). Figure 4. AZD8330 |
| Method | Western blot | |
| Cell Lines | osteosarcoma cell lines | |
| Concentrations | 0.5 μM | |
| Incubation Time | 6 h | |
| Results | The resistant cell lines KPD, ZK58 and Saos-2 showed no constitutive ERK activation. Exposing MOS, U2OS and 143b to a concentration of 0.5μM of Trametinib, AZD8330 or TAK-733 for 6 hours, led to loss of ERK phosphorylation indicating effective MEK inhibition |
| Cell Experiment | |
|---|---|
| Cell lines | HT-29, Malme-3M, MIA PaCa-2, BxPC3, BT474, Zr-75-1 and Malme-3 cell lines |
| Preparation method | Cellular viability assays Cells plated in 96-well plates were incubated with multiple concentrations of compound for 3 days. The number of viable cells was determined using the CellTiter 96 Aqueous Nonradioactive Cell Proliferation Assay (Promega, Madison, WI). |
| Concentrations | 0~50μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | HT-29 and BxPC3 xenograft |
| Formulation | 10 mL/kg and 10% ethanol/10% cremophor EL/80% D5W |
| Dosages | 10, 25, 50, or 100 mg/kg BID |
| Administration | oral |
| Molecular Weight | 461.23 |
| Formula | C16H17FIN3O4 |
| CAS Number | 869357-68-6 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Yao Yao, et al. Effect of AZD8330 on proliferation and apoptosis of multiple myeloma cells
[3] Caela R Miller, et al. MEK1/2 inhibitors in the treatment of gynecologic malignancies
[4] Akintunde Akinleye, et al. MEK and the inhibitors: from bench to bedside
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AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| CI-1040
CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. |
| ARRY-162 (Binimetinib)
ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. |
| TAK-733
TAK-733 is a potent and selective MEK allosteric site inhibitor with IC50 of 3.2nM for the treatment of cancer. |
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