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Selumetinib

CAT: 0013-GTR19161275-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161275-01Size:500 mg
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Description
A highly potent and selective, ATP-uncompetitive inhibitor of MEK1/2 with IC50/Ki of 14.1 nM/22.6 nM for MEK1; shows no activity against other 40 serine/threonine and tyrosine kinases; inhibits cellular ERK1/2 phosphorylation (IC50<40 nM), suppresses growth inhibition of several cell lines containing B-Raf and Ras mutations (IC50=59-473 nM) ; causes growth of HT-29 xenograft tumors in nude mice.Skin Cancer Approved (In Vitro) :Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells.Selumetinib (AZD6244) (1μM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells.Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line. (In Vivo) :Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model.
CAS Number
606143-52-6
Product Name Alternative
ARRY-142886 | AZD-6244
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 34 mg/mL
Smiles
O=C (C1=C (NC2=CC=C (Br) C=C2Cl) C (F) =C3C (N (C) C=N3) =C1) NOCCO
Molecular Formula
C17H15BrClFN4O3
Molecular Weight
457.6814
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1H-Benzimidazole-6-carboxamide, 5-[ (4-bromo-2-chlorophenyl) amino]-4-fluoro-N- (2-hydroxyethoxy) -1-methyl-

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FS27812-01Selumetinib
200300Selumetinib (AZD6244)
C03674-01Selumetinib sulfate
A8207-500AZD6244 (Selumetinib)
HY-50706R-01Selumetinib (Standard)

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