CAS 869357-68-6|AZD8330
Introduction：Basic information about CAS 869357-68-6|AZD8330, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | AZD8330 | ||
|---|---|---|---|
| CAS Number | 869357-68-6 | Molecular Weight | 461.227 |
| Density | 1.7±0.1 g/cm3 | Boiling Point | / |
| Molecular Formula | C16H17FIN3O4 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide |
|---|---|
| Synonym | More Synonyms |
AZD8330 BiologicalActivity
| Description | AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM. |
|---|---|
| Related Catalog | Research Areas >>Cancer |
| Target | MEK1:7 nM (IC50) MEK2:7 nM (IC50) |
| In Vitro | AZD8330 is a selective allosteric MEK1/ MEK2 inhibitor. Exposing human osteosarcoma cell lines MOS, U2OS, and 143B to a concentration of 0.5 μM of Trametinib, AZD8330 or TAK-733 for 6 hours, leads to loss of ERK phosphorylation indicating effective MEK inhibition.The activity of these three inhibitors is tested using concentration ranges in six osteosarcoma cell lines: MOS, U2OS, KPD, ZK58, 143b and Saos-2. All three inhibitors decrease viability of MOS and U2OS and strongly affect 143b. By contrast, viability of KPD, ZK58 and Saos-2 is not affected by any of the three inhibitors[2]. |
| In Vivo | In tumour xenograft models, AZD8330 demonstrates dose-dependent tumour growth inhibition of approximately 90% at tolerated doses (1.0 mg/kg once daily [OD])[1]. |
| Cell Assay | Human osteosarcoma cell lines MOS, U2OS, 143B, ZK58, KPD and Saos-2 are grown in RPMI1640 medium supplemented with 10% fetal bovine serum and 25 U/mL Penicillin and 25 μg/mL of Penicillin-Streptomycin. All cells are cultured in a humidified incubator at 37°C with 5% CO2. Dose response curves for Trametinib, AZD8330 (10 nM, 100 nM, and 1 μM) and TAK-733 in 6 osteosarcoma cell lines as indicated. Cells are exposed for 72 hours. Cells are processed using the ATPlite 1Step kit, followed by luminescence measurement on a plate reader[2]. |
| References | [1]. Cohen RB, et al. A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies. Eur J Cancer. 2013 May;49(7):1521-9. [2]. Baranski Z, et al. MEK inhibition induces apoptosis in osteosarcoma cells with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov;6(11-12):503-12. |
Chemical & Physical Properties
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Molecular Formula | C16H17FIN3O4 |
| Molecular Weight | 461.227 |
| Exact Mass | 461.024780 |
| PSA | 96.08000 |
| LogP | 2.05 |
| Index of Refraction | 1.659 |
| InChIKey | RWEVIPRMPFNTLO-UHFFFAOYSA-N |
| SMILES | Cc1cc(C(=O)NOCCO)c(Nc2ccc(I)cc2F)n(C)c1=O |
| Storage condition | -20°C |
Synonyms
| 2-(2-Fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide |
| AZD-8330 |
| S2134_Selleck |
| AZD8330 |
| ARRY-704 |
| 2-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide |
| 3-Pyridinecarboxamide, 2-[(2-fluoro-4-iodophenyl)amino]-1,6-dihydro-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo- |
| 2-[(2-Fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide |
| 2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide |
| AZD 8330 |
| UNII-G4990BOZ66 |
