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GSK1120212 (DMSO solvate)

GSK1120212 (DMSO solvate)
GSK1120212 (DMSO solvate) structure
CAS No.
1187431-43-1
Chemical Name:
GSK1120212 (DMSO solvate)
Synonyms
154988;JTP-74057;GSK 1120212B;JTP-74057;GSK1120212;TraMetinib DMSO (API);JTP-74057 (DMSO solvate);TraMetinib (DMSO solvate);GSK1120212 (DMSO solvate);rametinibdimethylsulfoxide;Trametinib dimethyl sulfoxide
CBNumber:
CB92624177
Molecular Formula:
C28H29FIN5O5S
Formula Weight:
693.5282332
MOL File:
1187431-43-1.mol

GSK1120212 (DMSO solvate) Properties

FDA UNII
BSB9VJ5TUT
NCI Dictionary of Cancer Terms
trametinib dimethyl sulfoxide
NCI Drug Dictionary
trametinib dimethyl sulfoxide

GSK1120212 (DMSO solvate) price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ApexBio Technology A3887 TrametinibDMSOsolvate 1187431-43-1 10mM (in 1mL DMSO) $55 2021-12-16 Buy
ChemScene CS-0061 Trametinib(DMSOsolvate) 99.77% 1187431-43-1 10mg $60 2021-12-16 Buy
Apolloscientific BISN0218 Trametinib DMSO solvate 1187431-43-1 5mg $68 2021-12-16 Buy
Biosynth Carbosynth FT65193 GSK 1120212B 1187431-43-1 50 mg $75 2021-12-16 Buy
ApexBio Technology A3887 TrametinibDMSOsolvate 1187431-43-1 50mg $80 2021-12-16 Buy

GSK1120212 (DMSO solvate) Chemical Properties,Uses,Production

Description

In May 2013, the US FDA approved trametinib (also referred to as GSK1120212 and JTP-74057), for the treatment of patients with unresectable or metastatic melanoma with BRAFV600e or BRAFV600K mutations as detected by an FDA-approved test. Extensive lead optimization led to the identification of trametinib which is a potent ATP noncompetitive inhibitor of MEK1 and MEK2 (IC50 =0.7 and 0.9 nM, respectively, with initially unphosphorylated MEK). It also showed inhibitory activity in ACHN and HT-29 cancer cell lines (IC50s of 9.8 and 0.57 nM, respectively). Consistent with its in vitro activity, trametinib showed significant antitumor activity in a KRASG12S A549 tumor xenograft model where near to complete tumor growth inhibition (TGI) was observed at 5.0 and 2.5 mg/kg (92% and 87% TGI, respectively). Broad antitumor activity was seen in other xenograft models as well. A synthetic route to trametinib that employs a base catalyzed rearrangement of a pyrido[2,3-d]pyrimidine core to pyrido[4,3-d]pyrimidine, as a key step has been reported.

Originator

Japan Tobacco (Japan)

Uses

Trametinib (DMSO Solvate) is a highly potent and selective MEK inhibitor with significant antitumor activity.

Definition

ChEBI: An addition compound obtained by combining equimolar amounts of trametinib and dimethyl sulfoxide. Used for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, and who have not received prior BRAF inhibito treatment.

brand name

Mekinist

Chemical Synthesis

Commercial 2-fluoro-4-iodoaniline (180) was sequentially subjected to CDI and cyclopropylamine to generate urea 181 in 96% yield. This was followed by coupling with cyanoacetic acid in the presence of mesyl chloride and DMF to furnish imide 182 in 96% yield. Under basic conditions, imide 182 underwent an intramolecular cyclization reaction to produce pyrimidine-2,4- dione 183 in 88% yield. Next, condensation with DMF–DMA generated formamidine 184 in 92% yield, and this was followed by NaBH4-mediated reduction and subsequent annulation with 2- methyl-malonic acid (186) to arrive at trione 187 in 58% from 184. Trione 187 was then treated with p-toluenesulfonyl chloride in Et3N, and the resulting tosylate was exposed to 30-aminoacetanilide (189) in the presence of 2,6-lutidine and DMA, inducing an addition-elimination reaction to give pyrido[2,3-d]pyrimidine 190 in 93% yield. The rearrangement of pyrido[2,3-d]pyrimidine 190 with sodium methoxide in THF/MeOH gave pyrido[4,3- d]pyrimidine (trametinib) in 89% yield. This was then complexed with a single equivalent of DMSO to produce trametinib DMSO (XXIV) in 92% yield.

GSK1120212 (DMSO solvate) Preparation Products And Raw materials

Raw materials

Preparation Products


GSK1120212 (DMSO solvate) Suppliers

Global( 88)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
AFINE CHEMICALS LIMITED
008657185134551
008657185134895 info@afinechem.com CHINA 15559 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
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+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60
HubeiwidelychemicaltechnologyCo.,Ltd
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Hubei xin bonus chemical co. LTD
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career henan chemical co
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Shaanxi Dideu Medichem Co. Ltd
15319487004
029-88380327 1015@dideu.com CHINA 3994 58
Target Molecule Corp
18019718960 781-999-5354
marketing@targetmol.com United States 19231 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
13588875226 86-571-88216897、88216896
86-571-88216895 sales@hzclap.com CHINA 6469 58

View Lastest Price from GSK1120212 (DMSO solvate) manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-04-28 GSK1120212 (DMSO solvate)
1187431-43-1
US $0.10 / KG 1KG 99.0% 1000 tons Shaanxi Dideu Medichem Co. Ltd
2020-02-26 Trametinib
1187431-43-1
US $0.00-0.00 / KG 100g 99.0%+ 100 tons Shaanxi Dideu Medichem Co. Ltd
2020-02-26 Trametinib
1187431-43-1
US $0.00-0.00 / KG 1KG 99.0%+ 100 tons Shaanxi Dideu Medichem Co. Ltd

1187431-43-1(GSK1120212 (DMSO solvate))Related Search:


  • GSK 1120212B
  • Trametinib dimethyl sulfoxide
  • GSK1120212 (DMSO solvate)
  • JTP-74057
  • TraMetinib (DMSO solvate)
  • TraMetinib DMSO (API)
  • GSK-1120212 dimethyl sulfoxide
  • N-(3-(3-cyclopropyl-5-((2-fluoro-4-iodophenyl)amino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acetamide compound with (methylsulfinyl)methane (1:1)
  • 154988
  • Trametinib DMSO solvate, >=98%
  • JTP-74057;GSK1120212
  • N-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-1H,2H,3H,4H,6H,7H-pyrido[4,3-d]pyrimidin-1-yl}phenyl)acetamide
  • JTP-74057 (DMSO solvate)
  • rametinibdimethylsulfoxide
  • 1187431-43-1
  • C28H29FIN5O5S
  • C26H23FIN5O4C2H6OS
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