GSK1120212 (DMSO solvate)

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

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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
color: White to off-white
InChI: InChI=1S/C26H23FIN5O4.C2H6OS/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34;1-4(2)3/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34);1-2H3
InChIKey: OQUFJVRYDFIQBW-UHFFFAOYSA-N
SMILES: S(=O)(C)C.N(C1C=CC(I)=CC=1F)C1N(C(=O)C(C)=C2N(C3C=CC=C(NC(=O)C)C=3)C(=O)N(C3CC3)C(=O)C=12)C

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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..…

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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

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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 BRAF^V600e or BRAF^V600K 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 (IC_50s of 9.8 and 0.57 nM, respectively). Consistent with its in vitro activity, trametinib showed significant antitumor activity in a KRAS^G12S 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

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View Lastest Price from GSK1120212 (DMSO solvate) manufacturers

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

Shaanxi Dideu Medichem Co. Ltd

Product: GSK1120212 (DMSO solvate) 1187431-43-1
Price: US $0.10/KG
Min. Order: 1KG
Purity: 99.0%
Supply Ability: 1000 tons
Release date: 2020-04-27

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

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

Trametinib Lenalidomide

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

DMSO solvate

Enzastaurin Impurity 1 (Bisindolylmaleimide V)

Trametinib Impurity 28

1187431-43-1

C28H29FIN5O5S

C26H23FIN5O4C2H6OS

API