Indications and Usage Mechanisms of Action Clinical Research
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Selumetinib

Indications and Usage Mechanisms of Action Clinical Research
Product Name
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;ARRY 142886;Selumetinib;Array142886
CBNumber
CB81871940
Molecular Formula
C17H15BrClFN4O3
Formula Weight
457.68
MOL File
606143-52-6.mol
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Selumetinib Property

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.
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Safety

HS Code 
29349990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H317May cause an allergic skin reaction

H318Causes serious eye damage

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P262Do not get in eyes, on skin, or on clothing.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
11599
Product name
AZD 6244
Purity
≥98%
Packaging
10mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
11599
Product name
AZD 6244
Purity
≥98%
Packaging
25mg
Price
$55
Updated
2024/03/01
Cayman Chemical
Product number
11599
Product name
AZD 6244
Purity
≥98%
Packaging
50mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
11599
Product name
AZD 6244
Purity
≥98%
Packaging
100mg
Price
$109
Updated
2024/03/01
Tocris
Product number
6815
Product name
Selumetinib
Purity
≥98%(HPLC)
Packaging
50
Price
$91
Updated
2021/12/16
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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.

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.

target

MEK1

storage

Store at -20°C

References

1) Davies?et al. (2007),?AZD6244(ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamics relationship, and potential for combination in preclinical models; Mol. Cancer Ther.,?6?2209 2) Yeh?et al. (2007),?Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor; Clin. Cancer Res.,?13?1576 3) Catalanotti?et al. (2013),?Phase II trial of MEK inhibitor selumetinib(AZD6244) in patients with BRAFV600E/K-mutated melanoma; Clin. Cancer Res.,?19?2257 4) O’Neil?et al. (2011),?Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma; J. Clin. Oncol.,?29?2350 5) Khurum?et al. (2012),?A phase I dose escalation study of oral MK-2206 (allosteric Akt inhibitor) with oral selumetinib (AZD6244)(MEK 1/2 inhibitor) in patients with advanced or metastatic solid tumors; J. Clin. Oncol.,?30?e13599 6) Hainsworth?et al. (2010),?A phase II, open label, randomized study to assess the efficacy and safety of AZD6244 versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens; J. Thorac. Oncol.,?5?1630 7) Bodoky?et al. (2012),?A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy; Invest. New Drugs,?30?1216

Selumetinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Selumetinib manufacturers

Hebei Mojin Biotechnology Co., Ltd
Product
Selumetinib 606143-52-6
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
50000KG/month
Release date
2023-06-21
Zhengzhou Anbu Chem Co.,Ltd
Product
Selumetinib 606143-52-6
Price
US $0.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1000KGS
Release date
2023-06-19
Hebei Guanlang Biotechnology Co., Ltd.
Product
Selumetinib 606143-52-6
Price
US $10.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10 mt
Release date
2021-08-06

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%
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  • Selumetinib USP/EP/BP
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  • Quinoxyfen Impurity 1
  • Selumetinib API
  • 606143-52-6
  • 60614-52-6
  • C17H15BrClFN4O3
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