ChemicalBook > CAS DataBase List > GSK1120212 (DMSO solvate)

GSK1120212 (DMSO solvate)

Product Name
GSK1120212 (DMSO solvate)
CAS No.
1187431-43-1
Chemical Name
GSK1120212 (DMSO solvate)
Synonyms
Trametinib dimethyl sulfoxide;154988;JTP-74057;GSK 1120212B;DMSO solvate;JTP-74057;GSK1120212;TraMetinib DMSO (API);Trametinib Impurity 28;JTP-74057 (DMSO solvate);GSK1120212 (DMSO solvate)
CBNumber
CB92624177
Molecular Formula
C28H29FIN5O5S
Formula Weight
693.53
MOL File
1187431-43-1.mol
More
Less

GSK1120212 (DMSO solvate) Property

storage temp. 
Store at -20°C
solubility 
insoluble in EtOH; insoluble in H2O; ≥11.2 mg/mL in DMSO with gentle warming and ultrasonic
form 
solid
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H317May cause an allergic skin reaction

H361Suspected of damaging fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P272Contaminated work clothing should not be allowed out of the workplace.

P273Avoid release to the environment.

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

P281Use personal protective equipment as required.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P363Wash contaminated clothing before reuse.

P391Collect spillage. Hazardous to the aquatic environment

P405Store locked up.

P501Dispose of contents/container to..…

More
Less

N-Bromosuccinimide Price

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

GSK1120212 (DMSO solvate) Chemical Properties,Usage,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

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¨CDMA 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

More
Less

GSK1120212 (DMSO solvate) Suppliers

Taizhou Ruixin Chemical Co., Ltd.
Tel
0576-89085261 15867635987
Fax
0576-89085262
Email
jasonhu09@163.com
Country
China
ProdList
442
Advantage
50
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696;
Email
info@hanhongsci.com
Country
China
ProdList
42982
Advantage
64
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9442
Advantage
58
Shenzhen HwaGen Pharmaceutical Co.,Ltd
Tel
0752-5538396 18927339850
Fax
0752-5319394
Email
sales1@rafflespt.com
Country
China
ProdList
216
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7553
Advantage
61
TargetMol Chemicals Inc.
Tel
021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7934
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3421
Advantage
58
Finetech Industry Limited
Tel
027-87465837 19945049750
Fax
027-8777-2287
Email
sales@finetechnology-ind.com
Country
China
ProdList
9636
Advantage
58
Shanghai HuanChuan Industry Co.,Ltd.
Tel
021-61478794
Fax
021-61478794
Email
sales@hcshhai.com
Country
China
ProdList
9798
Advantage
50
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4121
Advantage
55
Candia Pharmatech Co. , Ltd.
Tel
+86-371-55216238
Fax
+86-371-86615086
Country
China
ProdList
286
Advantage
60
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9254
Advantage
55
Shanghai Shanyuan pharmaceutical technology co., LTD
Tel
021-31761238 13167072949
Fax
021-31761238
Email
3146446224@qq.com
Country
China
ProdList
1609
Advantage
55
Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
Fax
020-61288700
Email
505721671@qq.com
Country
China
ProdList
3868
Advantage
58
Lancrix Chemicals
Tel
86-21-50817262
Fax
86-21-57712035
Email
sales@lancrix.com
Country
China
ProdList
1503
Advantage
55
ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8011
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2982
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
021-2022843681 15618226720
Fax
+86-21-51601218
Email
chaolaichem@foxmail.com
Country
China
ProdList
7565
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131981
Advantage
58
Hubei Yangxin Medical Technology Co., Ltd.
Tel
15374522761
Fax
QQ:2853117752
Email
3003392093@qq.com
Country
China
ProdList
7851
Advantage
55
Henan Anky Chemical Technology Co., Ltd.
Tel
17836913271
Fax
0374-8348899
Email
3224305243@qq.com
Country
China
ProdList
2707
Advantage
58
Chemleader Biomedical Co., Limited.
Tel
021-58180488
Fax
021-58180499
Email
sales@MedChemLeader.com
Country
China
ProdList
999
Advantage
58
Chengdu Saiousi Pharmaceutical Co., Ltd
Tel
028-64971018 18108168130
Fax
86 028-64971018
Country
China
ProdList
1781
Advantage
55
Shanghai Zhen Li Biological Technology Co., Ltd
Tel
021-16621358918; 18516310516
Fax
13045646768
Email
zhenlipharma888@163.com
Country
China
ProdList
1979
Advantage
58
Capot Chemical Co.,Ltd.
Tel
571-85586718 +8613336195806
Fax
+86-571-85864795
Email
sales@capotchem.com
Country
China
ProdList
29797
Advantage
60
Beijing Mesochem Technology Co., Ltd.
Tel
010-57862036 18811083386
Email
msales@mesochem.com
Country
China
ProdList
189
Advantage
58
Twochem Co.Ltd.
Tel
021-58111628 15800915896
Fax
QQ 3285589261
Country
China
ProdList
1988
Advantage
58
Wuhan NewBaiChuan Pharmaceutical Co., Ltd.
Tel
027-50476178
Fax
QQ644526144
Email
644526144@qq.com
Country
China
ProdList
418
Advantage
58
Nanjing crow LuNing pharmaceutical technology co., LTD
Tel
13382066392
Country
CHINA
ProdList
4880
Advantage
58
Angel Pharmatech, Ltd.
Tel
17317130613
Fax
QQ3358272972
Email
3358272972@qq.com
Country
China
ProdList
3238
Advantage
58
Shanghai Jizhi Biochemical Technology Co. Ltd.
Tel
400-400-400-9004166 18616739031
Email
3007523370@qq.com
Country
China
ProdList
52712
Advantage
58
Shanghai Pinbo Industrial Development Co. Ltd.
Tel
18321128505
Email
pinbochemical@163.com
Country
China
ProdList
161
Advantage
58
Wuhan Xinbaichuan Pharmaceutical Technology Co., Ltd.
Tel
027-50478167
Fax
QQ 252994272
Email
252994272@qq.com
Country
China
ProdList
277
Advantage
58
Jinan Guoding Pharmaceutical Technology Co., Ltd.
Tel
13153106106
Fax
053167801621
Email
sales@guodingpharma.com
Country
China
ProdList
481
Advantage
58
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9730
Advantage
58
Wuhan belka pharmaceutical co., LTD
Tel
17798255750
Email
2326587775@qq.com
Country
CHINA
ProdList
327
Advantage
58
Zhejiang J&C Biological Technology Co.,Limited
Tel
+1-2135480471 +1-2135480471
Email
sales@sarms4muscle.com
Country
China
ProdList
10523
Advantage
58
Finetech Industry Limited
Tel
+86-27-87465837 +8618971612321
Fax
86 27 87772287
Email
info@finetechnology-ind.com
Country
China
ProdList
9635
Advantage
58
Wuhan Fortuna Chemical Co., Ltd
Tel
+86-27-59207850 +86-13986145403
Fax
86-27-59524646
Email
info@fortunachem.com
Country
China
ProdList
5989
Advantage
58
Hefei TNJ Chemical Industry Co.,Ltd.
Tel
0551-65418684 +8618949823763
Fax
0086-551-65418684
Email
sales@tnjchem.com
Country
China
ProdList
25363
Advantage
58
Hefei Hirisun Pharmatech Co., Ltd
Tel
+8615056975894
Fax
86-0551-62678551
Email
shawn@hirisunpharm.com
Country
CHINA
ProdList
9923
Advantage
58
AFINE CHEMICALS LIMITED
Tel
0571-85134551
Fax
008657185134895
Email
info@afinechem.com
Country
CHINA
ProdList
15377
Advantage
58
Shanxi Xuanran Import and Export Trade Co., Ltd.
Tel
+8617735180244
Email
mike_yan@xuanranglobal.com
Country
CHINA
ProdList
4022
Advantage
58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Fax
86-571-88216895
Email
sales@hzclap.com
Country
CHINA
ProdList
6313
Advantage
58
Henan Weituxi Chemical Technology Co., Ltd.
Tel
0371-63284658; 18135795563
Fax
QQ:2885349392
Email
2885349392@qq.com
Country
China
ProdList
9997
Advantage
58
Chemwill Asia Co.,Ltd.
Tel
86-21-51086038
Fax
86-21-51861608
Email
chemwill_asia@126.com
Country
CHINA
ProdList
23931
Advantage
58
DC Chemicals
Tel
021-58447131 13564518121
Email
sales@dcchemicals.com
Country
China
ProdList
9414
Advantage
58
Wuhan Shuangjin Fine Chemical Co., Ltd.
Tel
027-51903003 15926256169
Fax
027-51903003
Email
773164315@qq.com
Country
China
ProdList
60
Advantage
58
HubeiwidelychemicaltechnologyCo.,Ltd
Tel
18627774460
Email
faith@widelychemical.com
Country
CHINA
ProdList
742
Advantage
58
More
Less

View Lastest Price from GSK1120212 (DMSO solvate) manufacturers

Henan Fengda Chemical Co., Ltd
Product
GSK1120212 (DMSO solvate) 1187431-43-1
Price
US $5.00-0.10/KG
Min. Order
1KG
Purity
98%
Supply Ability
g-kg-tons, free sample is available
Release date
2024-03-26
Senova Technology Co. Ltd.
Product
DMSO solvate 1187431-43-1
Price
US $0.00-0.00/g
Min. Order
1g
Purity
98%
Supply Ability
10KG
Release date
2023-12-14
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Trametinib dimethyl sulfoxide 1187431-43-1
Price
US $0.00/G
Min. Order
5G
Purity
98%min
Supply Ability
30kg/month
Release date
2023-02-07

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
  • TIANFU 1187431-43-1 GSK1120212 (DMSO solvate)
  • Trametinib dimethyl sulfoxide,GSK1120212 (DMSO solvate)
  • 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 dimethyl sulfoxide complex
  • Enzastaurin Impurity 1 (Bisindolylmaleimide V)
  • Trametinib Impurity 28
  • DMSO solvate
  • 1187431-43-1
  • C28H29FIN5O5S
  • C26H23FIN5O4C2H6OS