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Selumetinib, also known as AZD6244 or ARRY-142886, is a selective, non-ATP-competitive oral MEK1/2 inhibitor, which is used in the treatment of neurofibromatosis type I (NF-1) for children two years of age or older. Clinical trials of selumetinib for melanoma cancer, pancreatic cancer, colon cancer, lung cancer and breast cancer are also conducted by AstraZeneca in 2007.
CAS No. |
606143-52-6 |
Purity |
99.87% |
Target |
MEK |
IC50 |
12 nM , 14 nM |
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In Vitro |
Selumetinib leads to decrease in DNA synthesis and cell viability time-dependently and dose-dependently. Growth arrest and apoptosis are induced as well, accompanied with the inactivation of ERK in primary 2-1318 cells. |
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In Vivo |
Growth rate of 4-1318 xenografts is reduced by Selumetinib (50 and 100 mg/kg, p.o.) dose-dependently. At the dose of 50 mg/kg, Selumetinib also notably suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts. Selumetinib (10, 25, 50, or 100 mg/kg, p.o.) is able to inhibit both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. In a BxPC3 xenograft model, tumor regressions are deceted as well. |
Formula |
C₁₇H₁₅BrClFN₄O₃ |
SMILES |
O=C(C1=C(C(F)=C2N=CN(C2=C1)C)NC3=CC=C(C=C3Cl)Br)NOCCO |
M. Weight |
457.7 |
Storage |
Powder -20°C 3 years |
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Solvent & Solubility |
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Documentation |
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More Biological Information
http://www.medchemhub.com/
