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
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
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..…
N-Bromosuccinimide Price
- Product number
- A3887
- Product name
- TrametinibDMSOsolvate
- Packaging
- 10mM(in 1mL DMSO)
- Price
- $55
- Updated
- 2021/12/16
- Product number
- CS-0061
- Product name
- Trametinib(DMSOsolvate)
- Purity
- 99.77%
- Packaging
- 10mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- BISN0218
- Product name
- Trametinib DMSO solvate
- Packaging
- 5mg
- Price
- $68
- Updated
- 2021/12/16
- Product number
- FT65193
- Product name
- GSK 1120212B
- Packaging
- 50mg
- Price
- $75
- Updated
- 2021/12/16
- Product number
- A3887
- Product name
- TrametinibDMSOsolvate
- Packaging
- 50mg
- Price
- $80
- Updated
- 2021/12/16
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
GSK1120212 (DMSO solvate) Suppliers
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View Lastest Price from GSK1120212 (DMSO solvate) manufacturers
- 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
- 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
- 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