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);TraMetinib (DMSO solvate)
- CBNumber:
- CB92624177
- Molecular Formula:
- C28H29FIN5O5S
- Molecular Weight:
- 693.53
- MDL Number:
- MFCD21609250
- MOL File:
- 1187431-43-1.mol
- MSDS File:
- SDS
| 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 |
| 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 |
| NCI Dictionary of Cancer Terms | trametinib dimethyl sulfoxide |
| FDA UNII | BSB9VJ5TUT |
| NCI Drug Dictionary | trametinib dimethyl sulfoxide |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS08,GHS07,GHS09 |
|---|---|
| Signal word | Danger |
| Hazard statements | H361-H410-H317-H372 |
| Precautionary statements | P201-P202-P281-P308+P313-P405-P501-P261-P272-P280-P302+P352-P333+P313-P321-P363-P501-P260-P264-P270-P314-P501-P273-P391-P501 |
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 | 50mg | $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
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | sales@afinechem.com | China | 15377 | 58 |
| Shijiazhuang Dingmin Pharmaceutical Sciences Co., Ltd. | +86-0311-67591193 +8613931880626 | sales02@dingminpharma.com | China | 256 | 58 |
| Senova Technology Co. Ltd. | +86-0755-86703119 +8618503098836 | info@senovatech.com | China | 351 | 58 |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 20235 | 58 |
| Capot Chemical Co.,Ltd. | +86-（0）57185586718 +86-13336195806 | sales@capot.com | China | 29730 | 60 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21628 | 55 |
| Nanjing Finetech Chemical Co., Ltd. | 025-85710122 17714198479 | sales@fine-chemtech.com | CHINA | 885 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| HubeiwidelychemicaltechnologyCo.,Ltd | 18627774460 | faith@widelychemical.com | CHINA | 742 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22963 | 58 |
View Lastest Price from GSK1120212 (DMSO solvate) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2025-04-24 | Trametinib dimethyl sulfoxide
1187431-43-1
|
US $0.00 / G | 5G | 98%min | 30kg/month | WUHAN FORTUNA CHEMICAL CO., LTD | |
 |
2024-11-19 | Trametinib (DMSO solvate)
1187431-43-1
|
US $41.00-82.00 / mg | 99.71% | 10g | TargetMol Chemicals Inc. | ||
 |
2024-03-26 | GSK1120212 (DMSO solvate)
1187431-43-1
|
US $5.00-0.10 / KG | 1KG | 98% | g-kg-tons, free sample is available | Henan Fengda Chemical Co., Ltd |
-
- Trametinib dimethyl sulfoxide
1187431-43-1
- US $0.00 / G
- 98%min
- WUHAN FORTUNA CHEMICAL CO., LTD
-
- Trametinib (DMSO solvate)
1187431-43-1
- US $41.00-82.00 / mg
- 99.71%
- TargetMol Chemicals Inc.
-
- GSK1120212 (DMSO solvate)
1187431-43-1
- US $5.00-0.10 / KG
- 98%
- Henan Fengda Chemical Co., Ltd