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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Mitogen-activated protein kinase (MAPK) >MEK inhibitor >Trametinib

Trametinib

Trametinib Structure
  • ₹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
Manufacturer Product number Product description Packaging Price Updated Buy

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

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H317 May cause an allergic skin reaction Sensitisation, Skin Category 1 Warning GHS hazard pictograms P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H361 Suspected of damaging fertility or the unborn child Reproductive toxicity Category 2 Warning P201, P202, P281, P308+P313, P405,P501
H372 Causes damage to organs through prolonged or repeated exposure Specific target organ toxicity, repeated exposure Category 1 Danger GHS hazard pictograms P260, P264, P270, P314, P501
Precautionary statements:
P201 Obtain special instructions before use.
P202 Do not handle until all safety precautions have been read and understood.
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P272 Contaminated work clothing should not be allowed out of the workplace.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P281 Use personal protective equipment as required.
P302+P352 IF ON SKIN: wash with plenty of soap and water.
P308+P313 IF exposed or concerned: Get medical advice/attention.
P314 Get medical advice/attention if you feel unwell.
P321 Specific treatment (see … on this label).
P333+P313 IF SKIN irritation or rash occurs: Get medical advice/attention.
P363 Wash contaminated clothing before reuse.
P405 Store locked up.
P501 Dispose of contents/container to..…

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.

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