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AZD6244 (Selumetinib)

Catalog No.
A8207
MEK inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$94.00
In stock
100mg
$88.00
In stock
500mg
$297.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

AZD6244 is a highly potent and selective inhibitor of MEK1/2 with IC50 value of 14.1nM against MEK1 [1].

AZD6244 is a second generation MEK1/2 inhibitor. In the radioactive assay, AZD6244 shows potent inhibition against the purified MEK1without the competition with ATP. Besides, it is a selective inhibitor since it has no obvious inhibition against other tyrosine kinases including MKK6, EGFR, ErbB2 and B-Raf et al. In the cellular assay, AZD6244 inhibits the phosphorylation of ERK1/2 which are the direct substrates of MEK1/2. The IC50 value is 10.3nM. It also inhibits the EGF-induced phosphorylation of ERK1/2 but not ERK5 in A431 cells. Since MEK is important in cell proliferation, the block of MEK1/2 caused by AZD6244 leads to a growth inhibition in the cell lines containing activating B-Raf and Ras mutations with IC50 values ranging from 59 to 473nM. Furthermore, the administration of AZD6244 can significantly inhibit tumor growth both in the HT-29 xenograft model and the BxPC3 pancreatic tumor xenograft model [1].

References:
[1] Yeh TC, Marsh V, Bernat BA, Ballard J, Colwell H, Evans RJ, Parry J, Smith D, Brandhuber BJ, Gross S, Marlow A, Hurley B, Lyssikatos J, Lee PA, Winkler JD, Koch K, Wallace E. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res. 2007 Mar 1;13(5):1576-83.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt457.69
Cas No.606143-52-6
FormulaC17H15BrClFN4O3
Solubility≥22.88 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
SDFDownload SDF
Canonical SMILESCN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment: [1]

Cell lines

1205Lu cells (BRAFV600E)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

3 μM, 24 hours

Applications

Inhibition of cell growth by AZD6244 is caused by reversible G1 -phase cell cycle arrest. Adherent 1205Lu cells were treated with DMSO or 3 μM AZD6244 for 24 h or for 24 h and a further 24 h after removal of the drugs. Cells treated with AZD6244 were found to enter into the G1 -phase cell cycle arrest, but to reenter S phase after removal of the drug.
Animal experiment: [2]

Animal models

Nude mice implanted with HT-29 human colon carcinoma

Dosage form

Oral administration, 10, 25, 50, or 100 mg/kg, twice a day for 21 days

Applications

AZD6244 is effective in inhibiting tumor growth at all doses tested. The time to the tumor growth end point was 36 days for the two highest dose groups compared with 18 days for the vehicle control group. Tumor growth after 11 days of dosing was inhibited by 55% at the low dose of 10 mg/kg and by 70% at the high dose of 100 mg/kg. Recovery of tumor growth was observed after cessation of AZD6244 administration. Tumor regrowth was significantly delayed in the 100 mg/kg dose group.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Haass N K, Sproesser K, Nguyen T K, et al. The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxel. Clinical Cancer Research, 2008, 14(1): 230-239.

[2] Yeh T C, Marsh V, Bernat B A, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clinical Cancer Research, 2007, 13(5): 1576-1583.

Biological Activity

Description Selumetinib (AZD6244) is a potent, highly selective inhibitor of MEK1 with IC50 of 14 nM.
Targets MEK1          
IC50 14 nM          

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