Indications and Usage Mechanisms of Action Clinical Research
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Selumetinib

Indications and Usage Mechanisms of Action Clinical Research
Selumetinib Structure
Selumetinib
  • CAS No.606143-52-6
  • Chemical Name:Selumetinib
  • CBNumber:CB81871940
  • Molecular Formula:C17H15BrClFN4O3
  • Formula Weight:457.68
  • MOL File:606143-52-6.mol
Selumetinib Property
  • Density  :1.69
  • form  :Beige powder.
  • pka :14.20±0.10(Predicted)
  • FDA UNII :6UH91I579U
  • NCI Dictionary of Cancer Terms :AZD6244
  • ATC code :L01EE04
Safety
  • HS Code  :29349990
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
Selumetinib Price More Price(39)
  • Brand: Cayman Chemical
  • Product number: 11599
  • Product name : AZD 6244
  • Purity: ≥98%
  • Packaging: 10mg
  • Price: $25
  • Updated: 2021/12/16
  • Buy: Buy
  • Brand: Cayman Chemical
  • Product number: 11599
  • Product name : AZD 6244
  • Purity: ≥98%
  • Packaging: 25mg
  • Price: $43
  • Updated: 2021/12/16
  • Buy: Buy
  • Brand: Tocris
  • Product number: 6815
  • Product name : Selumetinib
  • Purity: ≥98%(HPLC)
  • Packaging: 50
  • Price: $91
  • Updated: 2021/12/16
  • Buy: Buy
  • Brand: TRC
  • Product number: S254000
  • Product name : Selumetinib
  • Purity: 
  • Packaging: 10mg
  • Price: $45
  • Updated: 2021/12/16
  • Buy: Buy
  • Brand: TRC
  • Product number: S254000
  • Product name : Selumetinib
  • Purity: 
  • Packaging: 100 mg
  • Price: $115
  • Updated: 2021/12/16
  • Buy: Buy

Selumetinib Chemical Properties,Usage,Production

  • Indications and Usage Selumetinib, 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 Action Selumetinib 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 Research In 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.
  • Description Selumetinib (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).
  • Uses It is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development. It is useful as biomarker in human lung cancer cell. Potent MEK inhibitor.
  • Uses It is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development.
  • Definition ChEBI: 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.
Selumetinib Preparation Products And Raw materials
Raw materials
Preparation Products
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606143-52-6, SelumetinibRelated Search:
  • ARRY 142886
  • AZD 6244
  • 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
  • 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
  • Selumetinib AZD624
  • 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-car
  • Selumetinib, 99%, a highly selective MEK1 inhibitor
  • Selumetinib, Free BaseAZD6244ARRY-142886
  • Selumetinib (AZD6244) Selumetinib
  • ARRY-142886; SELUMETINIB;AZD-6244;ARRY142886
  • AZD6244 (ARRY142886, Selumetinib)
  • AZD6244 (Selumetinib,ARRY-142886)
  • 113183
  • CS-1912
  • Selumetinib Base
  • Selumetinib
  • 5-(4-Bromo-2-chlorophenylamino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
  • 6-(4-Bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide
  • SeluMatinib(5-[(4-BroMo-2-chlorophenyl)aMino]-4-fluoro-N-(2-hydroxyethoxy)-1-Methyl-1H-benziMidazole-6-carboxaMide
  • AZD6244(SeluMetinib)
  • AZD6244; ARRY142886
  • SeluMetinib (AZD6244)
  • Array142886
  • AZD-6244(SeluMetinib)/AZD6244
  • 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carbox
  • AZD6244, ARRY-142886, ARRY-886
  • 5-(4-BroMo-2-chlorophenylaMino)-4-fluoro-1-Methyl-1H-benziMidazole-6-carbohydroxaMic acid 2-hydroxyethyl ester
  • 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide Selumetinib (AZD6244)
  • AZD 6244 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
  • selumetinib (MEK inhibitor)
  • Selumetinib, >=98%
  • AZD-6224
  • umetinib
  • umetinib (AZD6244) SeL
  • 1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-
  • Selumetinib USP/EP/BP
  • 606143-52-6
  • 60614-52-6
  • C17H15BrClFN4O3
  • MAPK
  • Inhibitors
  • Antineoplastic
  • apis
  • Aromatics
  • Heterocycles
  • Inhibitor
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API
  • Research