Selumetinib
- CAS No.
- 606143-52-6
- Chemical Name:
- Selumetinib
- Synonyms
- 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;113183;CS-1912;AZD 6244;AZD-6224;umetinib;Smetinib;ARRY 142886;Selumetinib
- CBNumber:
- CB81871940
- Molecular Formula:
- C17H15BrClFN4O3
- Molecular Weight:
- 457.68
- MOL File:
- 606143-52-6.mol
- Modify Date:
- 2024/5/21 15:15:33
| Melting point | >219°C (dec.) |
|---|---|
| Density | 1.69 |
| storage temp. | -20° |
| solubility | Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 2 mg/ml) |
| form | Beige powder. |
| pka | 14.20±0.10(Predicted) |
| color | White |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS05,GHS07,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H317-H318-H361d-H373 | |||||||||
| Precautionary statements | P262-P280-P312 | |||||||||
| HS Code | 29349990 | |||||||||
| NFPA 704 |
|
Selumetinib Chemical Properties,Uses,Production
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).
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.
brand name
Koselugo
General Description
Class: dual threonine/tyrosine kinase; Treatment: children with NF1; Other name: AZD-6244, ARRY-142886; Oral bioavailability = 62%; Elimination half-life = 6.2 h; Protein binding = 97.7%
Metabolism
Following oral administration of radiolabeled
selumetinib, the most prominent drug-related
component in the plasma was selumetinib,
accounting for 40% of the plasma radioactivity. The
major circulating metabolite was an amide
glucuronide 2, which accounted for 22% of the
plasma radioactivity. This metabolite resulted from loss of the ethanediol moiety to give the primary
amide 1, which underwent glucuronidation and an
additional loss of 2 mass units, most likely due to
further oxidation of the N-methylbenzimidazole
moiety (Fig. 5).
Dosage
Selumetinib is characterized by a moderate oral bioavailability (62%) and a relatively short half-life (6.2 h), and these properties contribute to twice-daily dosing regimen (25 mg dosage).
Selumetinib Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 | China | 12460 | 58 | Inquiry |
| Zhengzhou Anbu Chem Co.,Ltd | +86-0371-88006763; +8615988602810 | China | 3000 | 58 | Inquiry |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29897 | 58 | Inquiry |
| Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 | China | 8826 | 58 | Inquiry |