AZD6244 (Selumetinib), MEK Inhibitor

Selumetinib, also known as AZD6244, is an orally bioavailable small molecule with potential antineoplastic activity. Selumetinib inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells.

Product information

CAS Number: 606143-52-6

Molecular Weight: 457.68

Formula: C17H15BrClFN4O3

Chemical Name: 6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide

Smiles: CN1C=NC2=C(F)C(NC3=CC=C(Br)C=C3Cl)=C(C=C12)C(=O)NOCCO

InChiKey: CYOHGALHFOKKQC-UHFFFAOYSA-N

InChi: InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

AZD6244 was used at 5-10 µM final concentration in vitro and in cellular assays.

In Vivo:

AZD6244 was orally dosed to mice at 25-100 mg/kg once per day, or in combination with Docetaxel (15 mg/kg) or Irinotecan (25 mg/kg) to significantly reduce the tumor volume.

References:

1. Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. (2007) Clin Cancer Res. 13(5):1576-83.
2. Davies BR, et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. (2007) Mol Cancer Ther. 6(8):2209-19.
3. Dry JR, et al. Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244). (2010) Cancer Res. 70(6):2264-73.
4. Bhalla S, et al. The novel anti-MEK small molecule AZD6244 induces BIM-dependent and AKT-independent apoptosis in diffuse large B-cell lymphoma. (2011) Blood. 118(4):1052-61.

Products are for research use only. Not for human use.