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

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

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

Molarity Calculator

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 91 In-stock
Solution
10 mM * 1 mL in DMSO USD 91 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 260 In-stock
50 mg USD 390 In-stock
100 mg USD 620 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

AZD8330 Related Antibodies

Top Publications Citing Use of Products

View All MEK Isoform Specific Products:

View All Isoforms
MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

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].

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

AZD8330 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to pink

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (216.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.14%

SDS (584 KB)

COA (250 KB) LCMS (120 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1681 mL 10.8406 mL 21.6812 mL 54.2029 mL
5 mM 0.4336 mL 2.1681 mL 4.3362 mL 10.8406 mL
10 mM 0.2168 mL 1.0841 mL 2.1681 mL 5.4203 mL
15 mM 0.1445 mL 0.7227 mL 1.4454 mL 3.6135 mL
20 mM 0.1084 mL 0.5420 mL 1.0841 mL 2.7101 mL
25 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1681 mL
30 mM 0.0723 mL 0.3614 mL 0.7227 mL 1.8068 mL
40 mM 0.0542 mL 0.2710 mL 0.5420 mL 1.3551 mL
50 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0841 mL
60 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
80 mM 0.0271 mL 0.1355 mL 0.2710 mL 0.6775 mL
100 mM 0.0217 mL 0.1084 mL 0.2168 mL 0.5420 mL
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AZD8330 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD8330869357-68-6ARRY-424704 ARRY-704AZD 8330AZD-8330ARRY424704ARRY 424704ARRY704ARRY 704ARRY-704MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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