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Product Details
AZD6244 (Selumetinib),606143-52-6,IC-0224150
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].
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].
