1. MAPK/ERK Pathway
  2. MEK
  3. AZD8330

AZD8330 (Synonyms: ARRY-424704; ARRY-704)

Cat. No.: HY-12058 Purity: 99.14%
Handling Instructions

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

For research use only. We do not sell to patients.

AZD8330 Chemical Structure

AZD8330 Chemical Structure

CAS No. : 869357-68-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 768 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 6 publication(s) in Google Scholar

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Description

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

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

461.23

Formula

C₁₆H₁₇FIN₃O₄

CAS No.

869357-68-6

SMILES

IC1=CC(F)=C(C=C1)NC(N2C)=C(C=C(C2=O)C)C(NOCCO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (216.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (7.05 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.25 mg/mL (7.05 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3.25 mg/mL (7.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.14%

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Keywords:

AZD8330ARRY-424704 ARRY-704AZD 8330AZD-8330ARRY424704ARRY 424704ARRY704ARRY 704ARRY-704MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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AZD8330
Cat. No.:
HY-12058
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