Trametinib | MEK inhibitor

CAS:
871700-17-3
Catalog Number:
10-4759
Activity:
MEK inhibitor
Chemical Name:
N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide
Alternate Names:
GSK1120212
Molecular Weight:
615.39
Molecular Formula:
C26H23FIN5O4
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-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.
Shipping Code:
RT

Available Options

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10 mg$40.00
50 mg$150.00
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Trametinib (871700-17-3) is a highly potent (IC50 uMEK1 = 0.7 nM, pp-MEK1 = 14.9 nM)1 and selective MEK inhibitor displaying selective inhibition of proliferation in various BRAF mutant cancer cell lines (IC50 ACHN = 9.8 nM; IC50 HT-29 = 0.57 nM)2. It is approved for use against unresectable or metastatic BRAF-mutant melanoma alone or in combination with Dabrafenib.  Trametinib can limit outgrowth of tumors without directly inhibiting tumor cell proliferation via abrogation of cytokine-driven expansion of monocytic myeloid-derived suppressor cells (mMDSC) through a mechanism involving CD8+ T cells.3,4 Trametinib also displays potent anti-arthritic effects.5

References/Citations:

1) Gilmartin et al. (2011), GSK1120212 (JTP-74057) is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition; Clin. Cancer Res. 17 989
2) Abe et al. (2011), Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO solvate); ACS Med. Chem. Lett. 2 320
3) Allegrezza et al. (2016), Trametinib Drives T-cell-Dependent Control of KRAS Tumors by Inhibiting Pathological Myelopoiesis; Cancer Res. 76 6253
4) Vella et al. (2014), MEK inhibition, alone or in combination with BRAF inhibition, affects multiple functions of isolated normal human lymphocytes and dendritic cells; Cancer Immunol. Res. 2 351
5) Yamaguchi et al. (2012), Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide; Inflamm. Res. 61 445

CAS:
871700-17-3
Catalog Number:
10-4759
Activity:
MEK inhibitor
Chemical Name:
N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide
Alternate Names:
GSK1120212
Molecular Weight:
615.39
Molecular Formula:
C26H23FIN5O4
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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