GSK1120212 free base · Synonyms: Trametinib
Trametinib is an orally active MEK inhibitor of MEK1.
For research use only. Not for human or veterinary use.
GSK1120212 structure
CAS No.: 871700-17-3
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 500 mg | USD 410.00 | BP-02460-500mg | In stock | Get quote |
| 1 g | USD 650.00 | BP-02460-1g | In stock | Get quote |
| 2 g | USD 1,040.00 | BP-02460-2g | In stock | Get quote |
| 3 g | USD 1,250.00 | BP-02460-3g | In stock | Get quote |
| 5 g | USD 1,670.00 | BP-02460-5g | In stock | Get quote |
| 10 g | USD 2,680.00 | BP-02460-10g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis, cross the blood-brain barrier (BBB), used in research related to subarachnoid hemorrhage (SAH) .
Biological activity
In Vitro Trametinib (GSK1120212;JTP-74057) (0.1-100 nM) blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). Trametinib (JTP-74057) inhibits the growth of 9 out of 10 human colorectal cancer cell lines, and they shows cell-cycle arrest at the G1 phase after drug tratment. The combination of GSK2118436 and Trametinib (GSK1120212) effectively inhibits cell growth, decreases ERK phosphorylation, decreases cyclin D1 protein, and increases p27(kip1) protein in the resistant clones. In Vivo Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486. Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model. In a female Sprague-Dawley rat model of experimental subarachnoid hemorrhage (SAH) induced by autologous blood injection into the prechiasmatic cistern, trametinib (0.5 mg/kg, intraperitoneal injection, administered at 3, 9, and 24 hours after SAH induction) regulates cerebrovascular contractile function, significantly reduces the contractile response of the basilar artery to endothelin ET-1, decreases the maximum contractile amplitude of the middle cerebral artery to 5-CT, alleviates elevated intracranial pressure (ICP) in the subacute phase, improves neurological outcomes, and enhances overall health status without significant adverse effects.
Identifiers
- SMILES
-
CN1C(=O)C(C)=C2N(C(=O)N(C3CC3)C(=O)C2=C1NC1=CC=C(I)C=C1F)C1=CC(NC(C)=O)=CC=C1 - InChIKey
-
LIRYPHYGHXZJBZ-UHFFFAOYSA-N
Specifications
- MW (average)
- 615.3948
- Formula
- C26H23FIN5O4
- CAS No.
- 871700-17-3
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month;
Solubility
Soluble in DMSO