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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
Molecular Weight:
457.68
MDL Number:
MFCD11977472
MOL File:
606143-52-6.mol
Last updated:2023-06-30 15:45:59

Selumetinib Properties

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.
NCI Dictionary of Cancer Terms AZD6244
FDA UNII 6UH91I579U
ATC code L01EE04

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
GHS05,GHS07,GHS08
Signal word  Danger
Hazard statements  H317-H318-H361d-H373
Precautionary statements  P262-P280-P312
HS Code  29349990
NFPA 704
0
3 0

Selumetinib price More Price(41)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 10mg $32 2024-03-01 Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 25mg $55 2024-03-01 Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 50mg $86 2024-03-01 Buy
Cayman Chemical 11599 AZD 6244 ≥98% 606143-52-6 100mg $109 2024-03-01 Buy
Tocris 6815 Selumetinib ≥98%(HPLC) 606143-52-6 50 $91 2021-12-16 Buy
Product number Packaging Price Buy
11599 10mg $32 Buy
11599 25mg $55 Buy
11599 50mg $86 Buy
11599 100mg $109 Buy
6815 50 $91 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.

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

606093-58-7
606143-52-6
Synthesis of Selumetinib from Methyl 4-Amino-3-Fluoro-5-Nitro-2-(Phenylamino)Benzoate
Global( 310)Suppliers
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Hebei Mojin Biotechnology Co., Ltd
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025-85710122 17714198479 sales@fine-chemtech.com CHINA 885 55
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+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58

View Lastest Price from Selumetinib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Selumetinib pictures 2023-06-22 Selumetinib
606143-52-6
US $0.00 / KG 1KG 99% 50000KG/month Hebei Mojin Biotechnology Co., Ltd
Selumetinib pictures 2023-06-19 Selumetinib
606143-52-6
US $0.00 / KG 1KG 98% 1000KGS Zhengzhou Anbu Chem Co.,Ltd
SeluMetinib pictures 2022-02-18 SeluMetinib
606143-52-6
US $0.00 / gram 1gram 99% 10kg Zhejiang J&C Biological Technology Co.,Limited
  • Selumetinib pictures
  • Selumetinib
    606143-52-6
  • US $0.00 / KG
  • 99%
  • Hebei Mojin Biotechnology Co., Ltd
  • Selumetinib pictures
  • Selumetinib
    606143-52-6
  • US $0.00 / KG
  • 98%
  • Zhengzhou Anbu Chem Co.,Ltd
  • SeluMetinib pictures
  • SeluMetinib
    606143-52-6
  • US $0.00 / gram
  • 99%
  • Zhejiang J&C Biological Technology Co.,Limited

Selumetinib Spectrum

ARRY 142886 AZD 6244 Selumetinib AZD624 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-car 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 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 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 Selumetinib D4 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 5-((4-Bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzodimidazol-6-carboxamide Quinoxyfen Impurity 1 Selumetinib API 606143-52-6 60614-52-6 C17H15BrClFN4O3 MAPK Inhibitors Antineoplastic apis Aromatics Heterocycles Inhibitor Intermediates & Fine Chemicals Pharmaceuticals API Research