GSK1120212 (DMSO solvate)
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1.What is the GSK1120212 (DMSO solvate) ?
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.
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.
2.What is the CAS number for GSK1120212 (DMSO solvate) ?
The CAS number of GSK1120212 (DMSO solvate) is 1187431-43-1.
3.What are another words for GSK1120212 (DMSO solvate) ?
Synonyms?for?GSK1120212 (DMSO solvate) 1187431-43-1:Trametinib DMSO
4.What is GSK1120212 (DMSO solvate) (1187431-43-1) used for?
Trametinib (DMSO Solvate) is a highly potent and selective MEK inhibitor with significant antitumor activity.
Relevant articles related to GSK1120212 (DMSO solvate):
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5-AMINO-2,4,7-TRIOXO-3,4,7,8-TETRAHYDRO-2H-PYRIDO’2,3-D! PYRIMIDINE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER |
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5.Buy GSK1120212 (DMSO solvate) with the best price .
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