AZD8330

Modify Date: 2024-01-13 16:42:51

AZD8330 Structure
AZD8330 structure
Common Name AZD8330
CAS Number 869357-68-6 Molecular Weight 461.227
Density 1.7±0.1 g/cm3 Boiling Point N/A
Molecular Formula C16H17FIN3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZD8330


AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.

 Names

Name 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide
Synonym More Synonyms

 AZD8330 Biological Activity

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

[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
Storage condition -20°C

 Synthetic Route

~91%

AZD8330 Structure

AZD8330

CAS#: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

 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
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Price: $145/10mM*1mLinDMSO

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