869357-68-6
869357-68-6 structure
- Name: AZD8330
- Chemical Name: 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide
- CAS Number: 869357-68-6
- Molecular Formula: C16H17FIN3O4
- Molecular Weight: 461.227
- Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Dihydropyridine
- Create Date: 2017-04-10 04:49:24
- Modify Date: 2024-01-13 16:42:51
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AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
| Name | 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide |
|---|---|
| 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 |
| Description | AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM. |
|---|---|
| Related Catalog | |
| 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 |
| 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 |
| Storage condition | -20°C |
|
~91%
869357-68-6 |
| Literature: ARRAY BIOPHARMA INC.; ASTRAZENECA AB Patent: WO2007/44084 A2, 2007 ; Location in patent: Page/Page column 82; 83 ; WO 2007/044084 A2 |
