AZD8330 (ARRY704; ARRY424704)

Alias: ARRY704; AZD 8330; AZD8330; ARRY424704; ARRY-704; ARRY 424704; ARRY 704; ARRY-424704; AZD-8330
Cat No.:V0458 Purity: ≥98%
AZD8330 (AZD-8330; ARRY-704; ARRY-424704) is an orally bioactive and non-ATP competitive (Allosteric) MEK 1/2 inhibitor with potential anticancer activity.
AZD8330 (ARRY704; ARRY424704) Chemical Structure CAS No.: 869357-68-6
Product category: MEK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

AZD8330 (AZD-8330; ARRY-704; ARRY-424704) is an orally bioactive and non-ATP competitive (Allosteric) MEK 1/2 inhibitor with potential anticancer activity. It has an IC50 of 7 nM for MEK1/2 inhibition.

Biological Activity I Assay Protocols (From Reference)
Targets
MEK1 (IC50 = 7 nM); MEK2 (IC50 = 7 nM)
ln Vitro
AZD8330 is a selective allosteric MEK1/ MEK2 inhibitor. Loss of ERK phosphorylation indicates effective MEK inhibition when the human osteosarcoma cell lines MOS, U2OS, and 143B are exposed to 0.5 μM of trametinib, AZD8330, or TAK-733 for 6 hours. Six osteosarcoma cell lines—MOS, U2OS, KPD, ZK58, 143b, and Saos-2—are used to test the activity of these three inhibitors at different concentrations. All three inhibitors have a significant negative impact on 143b and reduce the viability of MOS and U2OS. However, none of the three inhibitors affect the viability of KPD, ZK58, or Saos-2[2].
ln Vivo
At tolerated doses (1.0 mg/kg once daily [OD]), AZD8330 exhibits a dose-dependent tumour growth inhibition of 90% in tumor xenograft models[1].
Enzyme Assay
MEK1 (S218D, S222D ΔR4F) is expressed in baculovirus-infected Hi5 insect cells and purified using immobilized metal affinity chromatography, ion exchange, and gel filtration. MEK1 is also NH2-terminally hexahistidine-tagged and constitutively active. When [γ- 33P]phosphate from [γ- 33P]ATP is incorporated onto ERK2, it is possible to measure the activity of MEK1 in the body. An incubation solution (100 μL) consisting of 25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-glycerolphosphate, 100 μM sodium orthovanadate, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, and 0 to 80 nM AZD8330 (final concentration of 1% DMSO) is used in the assay. The addition of 10 μM ATP (with 0.5 μC k[γ-33P]ATP/well) starts the reactions, which are then allowed to proceed for 45 min at room temperature. For the purpose of stopping the reaction and precipitating the proteins, an equal volume of 25% trichloracetic acid is added. The excess labeled ATP is removed with 0.5% phosphoric acid, the precipitated proteins are trapped on glass fiber B filter plates, and radioactivity is measured using a liquid scintillation counter. By changing the concentration of ATP in the reaction mixture, ATP dependence can be identified. The data have been fitted globally.
Cell Assay
Malme-3M melanoma cells are plated in 96-wells and subjected to AZD8330 treatments in a range of concentrations for an hour at 37 °C. Anti-phospho-ERK and anti-ERK 1/2 antibodies are incubated with the cells after they have been fixed and permeabilized. Secondary antibodies that have been fluorescently labeled are added after washing the plates. Utilizing a LICOR fluorescence imager, plates are examined. The total ERK signal is used to normalize the pERK signal.
Animal Protocol
Female nude rats (NIH rnu/rnu) with Calu-6 cells, nude rats with SW620 cells
0.3 mg/kg, 1 mg/kg
Oral administration
References

[1]. 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./a >

[2]. MEK inhibition induces apoptosis in osteosarcoma cells with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov;6(11-12):503-12.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H17FIN3O4
Molecular Weight
461.23
Exact Mass
461.02
Elemental Analysis
C, 41.67; H, 3.72; F, 4.12; I, 27.51; N, 9.11; O, 13.88.
CAS #
869357-68-6
Appearance
Solid powder
SMILES
CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO
InChi Key
RWEVIPRMPFNTLO-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H17FIN3O4/c1-9-7-11(15(23)20-25-6-5-22)14(21(2)16(9)24)19-13-4-3-10(18)8-12(13)17/h3-4,7-8,19,22H,5-6H2,1-2H3,(H,20,23)
Chemical Name
2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide
Synonyms
ARRY704; AZD 8330; AZD8330; ARRY424704; ARRY-704; ARRY 424704; ARRY 704; ARRY-424704; AZD-8330
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~92 mg/mL (~199.5 mM)
Water: <1 mg/mL
Ethanol: ~92 mg/mL (~199.5 mM)
Solubility (In Vivo)
0.5% hydroxyethyl cellulose+0.1% Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1681 mL 10.8406 mL 21.6812 mL
5 mM 0.4336 mL 2.1681 mL 4.3362 mL
10 mM 0.2168 mL 1.0841 mL 2.1681 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00454090 Completed Drug: AZD8330 Cancer AstraZeneca March 2007 Phase 1
Biological Data
  • AZD8330

    Selection of hits in two human osteosarcoma cell lines.2015 Nov;6(11-12):503-12.

  • AZD8330

    Validation of three MEK inhibitors in 6 osteosarcoma cell lines.2015 Nov;6(11-12):503-12.

  • AZD8330

    Validation of sensitivity to MEK inhibitors in a 3D culture system.2015 Nov;6(11-12):503-12.

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