| Name | Selumetinib sulfate |
| Description | Selumetinib sulfate (AZD6244 sulfate) is an orally available, selective and potent MEK1/2 inhibitor that inhibits MEK1/2 phosphorylation and may be useful for the study of symptomatic refractory fibroids in type 1 neurofibromatosis. |
| In vitro | Selumetinib sulfate (AZD6244) is a potent MEK inhibitor with an IC50 of 12 nM for purified MEK.Selumetinib sulfate is able to inhibit ERK1/2 phosphorylation in a variety of cancer cell lines with IC50s as low as 8 nM, both at basal and induced levels. In primary 2-1318 cells, Selumetinib sulfate induces growth arrest and apoptosis associated with ERK inactivation, resulting in reduced primary DNA synthesis and reduced cell viability over time and dose. [1]
In H-441 and H-1437 cells, Selumetinib sulfate (1 μM) exhibits antiproliferative effects by blocking the G0/G1 phase. [2]
In addition, Selumetinib sulfate inhibited the growth of various cell lines harboring B-Raf and Ras mutations, but had no significant effect on normal fibroblast cell lines. [3] |
| In vivo | In in vivo experiments, oral administration of 50 and 100 mg/kg Selumetinib sulfate dose-dependently reduced the growth rate of 4-1318 xenograft tumors; it also significantly inhibited the growth of 5-1318, 2-1318, 26-1004, and 29-1104 xenograft tumors at the 50 mg/kg dose. [1]
Oral administration of 10, 25, 50, or 100 mg/kg Selumetinib sulfate also inhibited ERK1/2 phosphorylation and reduced HT-29 xenograft tumor growth in nude mice. Meanwhile, tumor regression was observed in the BxPC3 xenograft model. [3] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.6 mM), Sonication is recommended.
DMSO : 40 mg/mL (71.97 mM), Sonication is recommended.
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| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
