Trametinib | MEK inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 10 mg | $40.00 | ||
| 50 mg | $150.00 |
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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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
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