Trametinib
- ₹0
- Product name: Trametinib
- CAS: 871700-17-3
- MF: C26H23FIN5O4
- MW: 615.39
- EINECS:
- MDL Number:MFCD17215075
- Synonyms: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 GSK-1120212;Trametinib free base;Mekinist trametinib;Trametinib (GSK1120212,JTP 74057);Trametinib, >=98%;CS-30;Trametinib Impurity;100836
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Properties
Melting point :300-301 °C
Density :1.74
storage temp. :-20°C
solubility :Soluble in DMSO (up to 20 mg/ml)
form :White solid.
pka :14.76±0.70(Predicted)
color :White
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.
InChI :InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
InChIKey :LIRYPHYGHXZJBZ-UHFFFAOYSA-N
SMILES :C(NC1=CC=CC(N2C3=C(C)C(=O)N(C)C(NC4=CC=C(I)C=C4F)=C3C(=O)N(C3CC3)C2=O)=C1)(=O)C
Density :1.74
storage temp. :-20°C
solubility :Soluble in DMSO (up to 20 mg/ml)
form :White solid.
pka :14.76±0.70(Predicted)
color :White
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.
InChI :InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
InChIKey :LIRYPHYGHXZJBZ-UHFFFAOYSA-N
SMILES :C(NC1=CC=CC(N2C3=C(C)C(=O)N(C)C(NC4=CC=C(I)C=C4F)=C3C(=O)N(C3CC3)C2=O)=C1)(=O)C
Safety Information
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Description
The dual specificity mitogen-activated protein kinase kinases (MEK) isoforms MEK1 and MEK2 function in a RAS/RAF/MEK/ERK signaling pathway to control cell growth, survival, and differentiation. Trametinib is a potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC50s = 0.7 and 0.9 nM, respectively). It shows specificity for MEK1/2 over a panel of more than 180 kinases, including B-Raf, c-Raf, and MEK5. Trametinib blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice. Trametinib, alone or in combination with other chemotherapeutic drugs, targets a subset of cancer cells that can be characterized by specific biomarkers, such as B-Raf, RAS, or CTNNB1 mutations.Related product price
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