GSK1120212 (DMSO solvate)

Base Information

• Chemical Name: GSK1120212 (DMSO solvate)
• CAS No.: 1187431-43-1
• Molecular Formula: C28H29FIN5O5S
• Molecular Weight: 693.5316
• Mol file: 1187431-43-1.mol

Synonyms:Trametinib DMSO

Chemical Property of GSK1120212 (DMSO solvate)

Chemical Property:

• PSA: 146.90000
• LogP: 5.52300
• Solubility.: insoluble in EtOH; insoluble in H2O; ≥11.2 mg/mL in DMSO with gentle warming and ultrasonic

Purity/Quality:

98%, ^*data from raw suppliers

TrametinibDMSOsolvate >98% ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

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

Technology Process of GSK1120212 (DMSO solvate)

There total 1 articles about GSK1120212 (DMSO solvate) which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

→ JTP-74057 dimethylsulfoxide solvate (1187431-43-1)

Guidance literature:

Refernces