All AbMole products are for research use only, cannot be used for human consumption.
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.
 |
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
| Related MEK Products |
|---|
| Balamapimod
Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity. |
| PD-334581
PD-334581 is a MEK1 inhibitor. |
| Tunlametinib
Tunlametinib, an antineoplastic agent, is a MEK1/2 inhibitor. |
| Glycinexylidide
Glycinexylidide (GX) is the active metabolite of Lidocaine. |
| Xantocillin
Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
