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Selumetinib

Indications and Usage Mechanisms of Action Clinical Research
Selumetinib
Selumetinib structure
CAS No.
606143-52-6
Chemical Name:
Selumetinib
Synonyms
113183;CS-1912;AZD 6244;AZD-6224;umetinib;ARRY 142886;Selumetinib;Array142886;Selumetinib Base;Selumetinib AZD624
CBNumber:
CB81871940
Molecular Formula:
C17H15BrClFN4O3
Formula Weight:
457.68
MOL File:
606143-52-6.mol

Selumetinib Properties

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
  • Risk and Safety Statements
HS Code  29349990

Selumetinib price More Price(39)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 10mg $25 2021-12-16 Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 25mg $43 2021-12-16 Buy
Tocris 6815 Selumetinib ≥98%(HPLC) 606143-52-6 50 $91 2021-12-16 Buy
TRC S254000 Selumetinib 606143-52-6 10mg $45 2021-12-16 Buy
TRC S254000 Selumetinib 606143-52-6 100 mg $115 2021-12-16 Buy

Selumetinib Chemical Properties,Uses,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 synthesis

606144-02-9
606143-52-6
Synthesis of Selumetinib from Methyl 5-(4-broMo-2-chlorophenylaMino)-4-fluoro-1-Methyl-1H-benzo[d]iMidazole-6-carboxylate

Selumetinib Preparation Products And Raw materials

Raw materials

Preparation Products


Selumetinib Suppliers

Global( 266)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jurong Coupling Biotechnology Co., Ltd.
13656108824
coupling278191416@hotmail.com CHINA 184 58
HONG KONG IPURE BIOLOGY CO.,LIMITED
18062405514 86 18062405514
ada@ipurechemical.com CHINA 3475 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29954 58
GIHI CHEMICALS CO.,LIMITED
08657186217390
sales@gihichemicals.com CHINA 310 58
Hebei Guanlang Biotechnology Co., Ltd.
+8619930503282
sales3@crovellbio.com China 5941 58
BOC Sciences
1-631-485-4226
1-631-614-7828 inquiry@bocsci.com United States 19752 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58

View Lastest Price from Selumetinib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-08-18 Selumetinib USP/EP/BP
606143-52-6
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
2021-08-07 Selumetinib
606143-52-6
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2021-07-13 Selumetinib
606143-52-6
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

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