AZD6244 (Selumetinib, ARRY-142886) is an orally active, highly potent and selective non-ATP competitive MEK inhibitor, inhibiting MEK1 with an IC50 of 14 nM. In vitro cell viability inhibition screening of a tumor cell line panel found that cell lines harboring BRAF or RAS mutations were more likely to be sensitive to AZD6244. Treatment of primary HCC cells with AZD6244 led to growth inhibition, caspase-3 and caspase-7 activation, poly(ADP)ribose polymerase cleavage, and inhibition of ERK1/2 and p90RSK phosphorylation. AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. Currently AZD6244 is undergoing Phase II/III clinical trials to treat solid tumors.
CAS Number: 606143-52-6
Molecular Weight: 457.68
Chemical Name: 6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide
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: ≥12 months 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
AZD6244 was used at 5-10 µM final concentration in vitro and in cellular assays.
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.
- 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.
- 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.
- Dry JR, et al. Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244). (2010) Cancer Res. 70(6):2264-73.
- 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.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.