成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

ChemicalBook--->CAS DataBase List--->606143-89-9

606143-89-9

606143-89-9 Structure

606143-89-9 Structure
IdentificationBack Directory
[Name]

Binimetinib
[CAS]

606143-89-9
[Synonyms]

MEK162
CS-394
ARRY 162
ARRY-162
ARRY-438162
Binimetinib
MEK162, ARRY-162
MEK162(Binimetinib)
MEK162 (ARRY-438162)
Binimetinib (MEK-162)
Binimetinib USP/EP/BP
Binimetinib ( Mektovi
Binimetinib(Free Base)
BINIMETINIB, ARRY-438162
Binimetinib,MEK162, ARRY-162
MEK162 (ARRY-162, ARRY-438162)
MEK162 (ARRY-438162,Binimetinib)
BiniMetinib (MEK162, ARRY-162, ARRY-438162)
1H-Benzimidazole-6-carboxamide,5-[(4-bromo-2-fluorophenyl)am...
ARRY 162; ARRY 438162; MEK-162;BINIMETINIB;MEK-162; ARRY-162; ARRY-438162
5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-car
5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methylbenzimidazole-6-carboxamide
5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-
5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
ARRY-438162 5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide Binimetinib (MEK162, ARRY-162, ARRY-438162)
[Molecular Formula]

C17H15BrF2N4O3
[MDL Number]

MFCD22124525
[MOL File]

606143-89-9.mol
[Molecular Weight]

441.227
Chemical PropertiesBack Directory
[Melting point ]

>203oC (dec.)
[density ]

1.67
[storage temp. ]

-20°C
[solubility ]

Soluble in DMSO (up to at least 25 mg/ml)
[form ]

solid
[pka]

14.20±0.10(Predicted)
[color ]

White
[Stability:]

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety DataBack Directory
[HS Code ]

2933998090
Questions And AnswerBack Directory
[Kinase inhibitor]

Binimetinib, also known as Mektovi, is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor with potential antineoplastic activity.
Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor.
[Mechanism of Action]

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cellfree assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.
[Pharmacokinetics]

The primary metabolic pathway is glucuronidation with UGT1A1 contributing up to 61% of the binimetinib metabolism. Other pathways of binimetinib metabolism include N-dealkylation, amide hydrolysis, and loss of ethane-diol from the side chain. The active metabolite M3 produced by CYP1A2 and CYP2C19 represents 8.6% of the binimetinib exposure. Following a single oral dose of 45 mg radiolabeled binimetinib, approximately 60% of the circulating radioactivity AUC in plasma was attributable to binimetinib.
[Binding Mode]

As shown in the co-crystal structure of binimetinib in complex with BRAF–MEK1 kinases and AMP–PNP (Fig. 1), the imine nitrogen of the benzo[d]imidazole core hydrogen bonds to both the amide NH of Ser212 and amide NH of Val211, and the amide oxygen also forms a hydrogen bond with the primary amine of Lys97. In addition, the terminal hydroxyl group hydrogen bonds to the α-phosphate oxygen of AMP–PNP. Also, the carboxamide side chain oxygen interacts indirectly with the carboxylic acid of Asp208 and AMP–PNP via a water molecule (Fig. 2).
Figure 1. Co-crystal structure of binimetinib and  AMP-PNP with BRAF–MEK1 (PDB ID: 7M0U).Figure 2. Summary of binimetinib and AMP–PNP  with BRAF–MEK1. interactions based on an X-ray  co-crystal structure.
Hazard InformationBack Directory
[Description]

Binimetinib (606143-89-9) is a potent (IC50?= 12 nM) and selective allosteric inhibitor of MEK1/2.1,2?Recently approved by the FDA for treatment of melanoma in combination with Encorafenib. Binimetinib has had limited success as monotherapy but has shown promise in combination with other chemotherapeutic agents.3-5
[Uses]

Binimetinib is a potent inhibitor of MEK1/2 with an IC50 of 12 nM in a cell-free assay.
[Definition]

ChEBI: Binimetinib is 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-fluorophenyl)nitrilo, and N-(2-hydroxyethoxy)aminocarbonyl groups, respectively. It is a MEK1 and MEK2 inhibitor (IC50= 12 nM). Approved by the FDA for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation in combination with encorafenib. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of benzimidazoles, a member of bromobenzenes, a member of monofluorobenzenes, a hydroxamic acid ester and a secondary amino compound.
[Brand name]

Mektovi
[General Description]

Class: dual threonine/tyrosine kinase; Treatment: melanoma with BRAF mutations; Other name: ARRY-162; Oral bioavailability = 50%; Elimination half-life = 3.5 h; Protein binding = 97%
[Enzyme inhibitor]

This MEK inhibitor (FW = 441.23 g/mol; CAS 606143-89-9; Solubility: 88 mg/mL DMSO, when warmed), also named MEK162, ARRY-162, ARRY- 438162, and 5- ( (4-bromo-2-fluorophenyl) amino) -4-fluoro-N- (2-hydroxy- ethoxy) -1-methyl-1H-benzo[d]imidazole-6-carboxamide, targets Mitogen- Activated Protein Kinase Kinase (MAPKK), also known as MAP2K and MEK, which phosphorylates Mitogen-Activated Protein Kinase (MAPK). (IC50 = 12 nM) and is the first targeted therapy to show activity in patients with NRAS -mutated melanoma.
[target]

MEK1
[References]

1) Lee?et al.?(2010),?Preclinical development of ARRY-162, a potent and selective MEK1/2 inhibitor;?Cancer Res.?70?2515 2) Winski?et al.?(2010),?MEK162 (ARRY-162), a novel MEK ? inhibitor, inhibits tumor growth regardless of KRAS/RAF pathway mutations;?EJC Supplements?8?56 3) Lee?et al.?(2016),?Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models;?Oncotarget?7?39595 4) Gong?et al.?(2017),?MEK162 Enhances Antitumor Activity of 5-Fluorouracil and Trifluridine in KRAS-mutated Human Colorectal Cancer Cell Lines;?Anticancer Res.?37?2831 5) Van Cutsem?et al.?(2019),?Binimetinib, Encorafenib, and Cetuximab Triplet Therapy for Patients With BRAF V600E-Mutant Metastatic Colorectal Cancer: Safety Lead-In Results From Phase III BEACON Colorectal Cancer study;?J. Clin. Oncol.?180?2459
Spectrum DetailBack Directory
[Spectrum Detail]

Binimetinib(606143-89-9)1HNMR
606143-89-9 suppliers list
Company Name: BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Tel: +86-18600796368 +86-18600796368 , +86-18600796368
Website: http://www.sjar-tech.com/
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: +86-0371-55170693 +86-19937530512 , +86-19937530512
Website: https://www.tianfuchem.com/
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: +undefined-21-51877795
Website: www.atkchemical.com
Company Name: career henan chemical co
Tel: +86-0371-86658258 +8613203830695 , +8613203830695
Website: www.coreychem.com/
Company Name: Biochempartner
Tel: 0086-13720134139
Website: www.biochempartner.com
Company Name: Jinan Carbotang Biotech Co.,Ltd.
Tel: +8615866703830 , +8615866703830
Website: http://www.is0513.com/ShowSupplierProductsList31189/0.htm
Company Name: Hubei xin bonus chemical co. LTD
Tel: 86-13657291602
Website: www.is0513.com/ShowSupplierProductsList1549548/0.htm
Company Name: BOC Sciences
Tel: +1-631-485-4226
Website: www.bocsci.com/
Company Name: Chongqing Chemdad Co., Ltd
Tel: +86-023-6139-8061 +86-86-13650506873 , +86-86-13650506873
Website: http://www.chemdad.com/
Company Name: TargetMol Chemicals Inc.
Tel: +1-781-999-5354 +1-00000000000 , +1-00000000000
Website: https://www.targetmol.com/
Company Name: ANHUI WITOP BIOTECH CO., LTD
Tel: +8615255079626 , +8615255079626
Website: www.is0513.com/showsupplierproductslist418627/0_en.htm
Company Name: Dideu Industries Group Limited
Tel: +86-29-89586680 +86-15129568250 , +86-15129568250
Website: https://www.dideu.com
Company Name: Baoji Guokang Bio-Technology Co., Ltd.
Tel: 0917-3909592 13892490616 , 13892490616
Website: http://www.gk-bio.com
Company Name: Shenzhen Shengda Pharma Limited
Tel: 755-85269922 +8613424394241 , +8613424394241
Website: www.shengdapharm.com
Company Name: Dayang Chem (Hangzhou) Co.,Ltd.
Tel: 571-88938639 +8617705817739 , +8617705817739
Website: https://www.dycnchem.com/
Company Name: Zhejiang J&C Biological Technology Co.,Limited
Tel: +1-2135480471 +1-2135480471 , +1-2135480471
Website: https://www.sarms4muscle.com
Company Name: CR Corporation Limited
Tel: +8613062833949 , +8613062833949
Website: http://www.crcorporation.cn/
Company Name: Hong Kong Excellence Biotechnology Co., Ltd.
Tel:
Website: www.is0513.com/showsupplierproductslist1274886/0.htm
Tags:606143-89-9 Related Product Information
1185763-69-2 639089-54-6 1037624-75-1 675576-98-4 356559-20-1 371942-69-7 1174046-72-0 439239-90-4 875444-08-9 875446-37-0 851983-85-2 1231930-82-7 1236699-92-5 606143-52-6 1032350-13-2 391210-10-9 871700-17-3 763113-22-0

This site uses cookies
This website uses cookies and similar technologies to store and retrieve information about your use of this website. This information helps us to provide, analyse and improve our services, which may include personalised content or advertising. We may share this information with Google and other third parties. This cookies are necessary for our website to work properly . By clicking "Continue" or continuing to browse our site you are agreeing to our and our partners use of cookies.
Accept