|Solubility||Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.|
|Declaration||Manufactured by SynKinase.|
|Other Product Data||
Target: mTOR | Kinase Group: Atypical (PIKK) | Substrate: Serine-Threonine
Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
Selumetinib (AZD6244) is a second-generation, orally available, potent and selective ATP non-competitive inhibitor of MEK 1/2. In direct assays, AZD6244 selectively inhibits purified active MEK1 and MEK2 with an IC(50) of 14nM, and AZD6244 has reported IC(50) values of < 100nm for MEK1 in ELISA assays and in bindings assays against recombinant domains of MEK2, Kd values were 53nM for AZD6244. AZD6244 demonstrated very effective anti-proliferation effects against several different cell lines with IC(50) values ranging from a low of 3nM to < 1µM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC(50) concentrations < 40nM. AZD6244 has demonstrated potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin, and lung cancer, and inhibition of tumor growth was found to correlate with the reduction of phospho-ERK1/2 levels in tumors.
- Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor: T.C. Yeh, et al.; Clin. Cancer. Res. 13, 1576 (2007)
- Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories: I.V. Hartung, et al.; Bioorg. Med. Chem. Lett. 23, 2384 (2013)