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
- MOL File:
- 1187431-43-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/25 20:04:46
| 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 |
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) 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.
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.
GSK1120212 (DMSO solvate) Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| MSN LABORATORIES PRIVATE LTD | +91 40 30438600 | New Delhi, India | 230 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15395 | 58 | Inquiry |
| Shijiazhuang Dingmin Pharmaceutical Sciences Co., Ltd. | +86-0311-67591193 +8613931880626 | China | 251 | 58 | Inquiry |
| Senova Technology Co. Ltd. | +86-0755-86703119 +8618503098836 | China | 351 | 58 | Inquiry |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | China | 20294 | 58 | Inquiry |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21667 | 55 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |