Selumetinib is an oral, potent selective mitogen activated protein kinase kinase (MEK) inhibitor, which has been shown to be effective against MEK-dependent tumours. It is intended to treat metastatic uveal melanoma, a rare malignancy that affects the eyes. It is the most common adult intraocular tumour; it arises from melanocytes in the uvea and affects mostly those from White ethnic groups, particularly those with light coloured irises.
- Density 1.69
- form Beige powder.
- HS Code 29349990
- Indications and UsageSelumetinib, 1 has a chemical name of 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide. It was developed by British company AstraZeneca and is used to treat advanced non-small cell lung cancer (NSCLC). It is mainly used to treat bile duct cancer, colon cancer, NSCLC, etc. Currently, Selumetinib is in stage III clinical trials for treatment of NSCLC.
- Mechanisms of ActionSelumetinib is the first mitogenextracellular kinase (MEK1/2) inhibitor to be used in thyroid cancer clinical trials. It inhibits extracellular signal regulating kinase (ERK/2) and activates caspase to dramatically inhibit ERK1/2 phosphorylation.
- Clinical ResearchIn phase II clinical trials of radioiodine-refractory papillary thyroid carcinoma, 39 patients took daily oral doses of Selumetinib (100mg bid) for 28 days; results showed that 21 patients’ conditions stabilized (54%), 11 patients’ conditions worsened (28%), 49% patients’ conditions were stable for 16 weeks, 36% patients’ conditions were stable for 24 weeks, and survival terms did not progress to 32 weeks. Negative reactions mainly consisted of rashes (59%), diarrhea (44%), and weakness (41%). Some studies found that after treating 20 patients with thyroid cancer with Selumetinib (75mg bid) for 4 weeks, Selumetinib increased the iodine uptake and retention of patients with radioiodine-refractory papillary thyroid carcinoma. In a blind and random comparative study between a Selumetinib and Docetaxel (DOC) combination treatment group and DOC and placebo treatment group for 87 mutant NSCLSC patients, survival times were 9.4 months and 5.2 months, PFS were 5.3 months and 2.1 months, RR were 37% and 0%, thus showing dramatic differences. Selumetinib’s main negative reactions include neutrophil depletion, dermatitis, and respiratory failure.
- DescriptionSelumetinib (AZD6244; ARRY-142886) is an oral MEK inhibitor. In a randomized trial, NSCLC patients with wild-type KRAS were randomized to erlotinib alone or combination therapy with selumetinib, while mutant KRAS patients were randomized to selumetinib alone or combination therapy. The primary end points were PFS for the KRAS wild-type cohort and objective response rate (ORR) for the KRAS mutant cohort. Results were not impressive, with no PFS difference in the KRAS wild-type arm (2.4 vs. 2.1?months) and no ORR difference in the KRASmutated subgroup (0% vs. 10%). A planned trial of selumetinib in combination with the anti-PD-L1 antibody durvalumab has since been suspended (NCT03004105).
- UsesIt is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development.
- DefinitionChEBI: A member of the class of benzimidazoles that is 1-methyl-1H-benzimidazole which is substituted at positions 4, 5, and 6 by fluorine, (4-bromo-2-chlorophenyl)amino, and N-(2-hydroxyethoxy)aminocarbonyl groups, respectiv ly. It is a MEK1 and MEK2 inhibitor.
- Dabrafenib Ceritinib (LDK378) Cabozantinib Dacomitinib (PF299804) WZ4002 1110813-31-4 AP26113 Lenvatinib Afatinib (BIBW 2992) Vandetanib AZD-6244 O-(2-(vinyloxy)ethyl)hydroxylamine Bortezomib MK-2206 2HCl PD 0325901 Trametinib Erlotinib hydrochloride N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide
- Company Name:Wuhan belka pharmaceutical co., LTD Gold
- Products Intro:Product Name:AZD6244司美替尼
Purity:99% HPLC Package:1g，5g，10g，50g，100g，500g;1000g
- Company Name:Wuhan Shuangjin Fine Chemical Co., Ltd. Gold
- Products Intro:Product Name:AZD6244
Purity:99% Package:10G 100G 500G
- Company Name:Hubei Junxian Biotechnology Co., Ltd Gold
- Products Intro:Product Name:Selumetinib
- Company Name:Jurong Coupling Biotechnology Co., Ltd. Gold
- Products Intro:Product Name:Selumetinib
- Company Name:Ningbo Risheng Pharmaceutical Technology Co., Ltd. Gold
- Products Intro:Product Name:Selumetinib;AZD6244
Purity:99%+ HPLC Remarks:kg