871700-17-3
N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide
CAS: 871700-17-3
Molecular Formula: C26H23FIN5O4
871700-17-3 - Names and Identifiers
871700-17-3 - Physico-chemical Properties
| Molecular Formula | C26H23FIN5O4 |
| Molar Mass | 615.39 |
| Density | 1.74 |
| Melting Point | 300-301 °C |
| Solubility | Soluble in DMSO (up to 20 mg/ml) |
| Appearance | White solid. |
| Color | White |
| pKa | 14.76±0.70(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Use | Trametinib (GSK1120212) is a highly specific and effective MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM and no inhibitory activity on c-Raf, B- Raf, ERK1/2. |
| In vitro study | GSK1120212 inhibits phosphorylation of MBP with an IC50 at 0.92 nM-3.4 nM for different subtypes of Raf and MEK. GSK1120212 had no inhibitory effect on the kinase activity of c-Raf, B- Raf, ERK1 and erk2. In addition, GSK1120212 did not have a strong inhibitory effect on the other 98 kinases. GSK1120212 has a strong inhibitory effect on human colon cancer cell lines, in which HT-29 and COLO205 cells constitutively express the active B- Raf mutation, and these two cells are the most sensitive to GSK1120212, the IC50 is 0.48 nM and 0.52 nM, respectively. The sensitivity of the cell line containing the k-Raf mutation to GSK1120212 ranged from 2.2 to 174 nM. In contrast, both B- Raf and K-Ras were wild-type in COLO320 DM cells and thus resistant to GSK1120212 even at 10 μm. Treatment with GSK1120212 for 24 hours induced cell cycle arrest in G1 phase in all sensitive cells. Consistent with this, GSK1120212 treatment resulted in p15 GSK1120212 inhibition of tumor necrosis factor-α and interleukin-6 production by peripheral blood mononuclear cells in most human colon cancer cell lines. |
| In vivo study | Oral administration of GSK1120212 at a dose of 0.3 mg/kg or 1 mg/kg (once a day for 14 days) was effective in inhibiting HT-29 tumors, and a dose of 1 mg/kg completely inhibited tumor growth. In cancer tissues, a single oral dose of 1 mg/kg GSK1120212 completely inhibited ERK1/2 phosphorylation, after 14 days, GSK1120212 at a dose of 0.1 mg/kg that could increase p15 completely inhibited adjuvant arthritis (AIA) and type II collagen-induced arthritis (CIA) in Lewis rats or DBA1/J mice. |
871700-17-3 - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29339900 |
871700-17-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.625 ml | 8.125 ml | 16.25 ml |
| 5 mM | 0.325 ml | 1.625 ml | 3.25 ml |
| 10 mM | 0.162 ml | 0.812 ml | 1.625 ml |
| 5 mM | 0.032 ml | 0.162 ml | 0.325 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Trametinib (GSK1120212) Visit Supplier Webpage Request for quotationCAS: 871700-17-3
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Mobile: 18021002903
QQ: 3008007409
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Spot supply
Product Name: Trametinib Visit Supplier Webpage Request for quotationCAS: 871700-17-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Trametinib (GSK1120212) Visit Supplier Webpage Request for quotationCAS: 871700-17-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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