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MedKoo Cat#: 201458 | Name: Trametinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Trametinib, also known as GSK1120212, is a n orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. On May 29, 2013, FDA approved T rametinib.

Chemical Structure

Trametinib
Trametinib
CAS#871700-17-3

Theoretical Analysis

MedKoo Cat#: 201458

Name: Trametinib

CAS#: 871700-17-3

Chemical Formula: C26H23FIN5O4

Exact Mass: 615.0779

Molecular Weight: 615.39

Elemental Analysis: C, 50.74; H, 3.77; F, 3.09; I, 20.62; N, 11.38; O, 10.40

Price and Availability

Size Price Availability Quantity
50mg USD 150.00 Ready to ship
100mg USD 250.00 Ready to ship
200mg USD 450.00 Ready to ship
1g USD 1,250.00 Ready to ship
5g USD 4,250.00 Ready to ship
10g USD 6,950.00 Ready to Ship
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Related CAS #
871700-17-3 1187431-43-1 (DMSO)
Synonym
GSK 1120212 GSK1120212; GSK-1120212; JTP74057; Trametinib. Brand name: Mekinist.
IUPAC/Chemical Name
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
InChi Key
LIRYPHYGHXZJBZ-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
CC(NC1=CC=CC(N(C(C(C(N2C3CC3)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)C2=O)=C1)=O
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
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 Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Antitumor activities: . Trametinib (JTP-74057) strongly inhibited MEK1/2 kinase activities, but did not inhibit another 98 kinase activities. Treatment by JTP-74057 resulted in growth inhibition accompanied with upregulation of p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. Daily oral administration of JTP-74057 for 14 days suppressed tumor growth of HT-29 and COLO205 xenografts in nude mice. Notably, tumor regression was observed only in COLO205 xenografts, and COLO205 was much more sensitive to JTP-74057-induced apoptosis than HT-29 in vitro. Treatment with an Akt inhibitor enhanced the JTP-74057-induced apoptosis in HT-29 cells. Finally, JTP-74057 exhibited an additive or a synergistic effect in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. JTP-74057, a highly specific and potent MEK1/2 inhibitor, exerts favorable antitumor activities in vitro and in vivo. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor. These results suggest the usefulness of JTP-74057 in therapeutic applications for colorectal cancer patients. (source: Int J Oncol. 2011 Jul;39(1):23-31).      
Biological target:
Trametinib (GSK1120212; JTP-74057) is an MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM.
In vitro activity:
Interestingly, several IAV (Influenza A virus)-induced cytokines were reduced on mRNA level in presence of Trametinib (Fig. 4A and B). The expression of IFNβ and the interferon stimulated gene (ISG) MxA was only found to be reduced by Trametinib in infected cells (Fig. 4A), but not strongly affected in vRNA-transfected cells (Fig. 4C). The results indicate that the cellular IFN response is not directly limited by Trametinib. Rather it seems to be primarily indirectly affected by reduced viral replication than being directly caused by deregulation of the Raf/MEK/ERK signaling cascade. Indeed, expression of IFNβ and MxA are not yet described to be directly regulated by the Raf/MEK/ERK signaling cascade. Considering Trametinib as antiviral drug it is beneficial that Trametinib does not directly alter the IFN response which is an important arm of cellular antiviral defense. A clearly decreased induction by Trametinib was also detectable for IL6, CCL5 and CXCL10 mRNA expression, which were induced by infection with PR8M/H1N1 (Fig. 4B). Reference: Mol Cancer Ther. 2016 Jan;15(1):172-83. https://pubmed.ncbi.nlm.nih.gov/29990517/
In vivo activity:
This study examined the mechanism by which trametinib impacts T-cell subpopulations after islet transplantation. T-cell subpopulations isolated from the liver and spleen of recipient mice on day 7, which were treated with vehicle or with 0.1 or 0.3 mg/kg trametinib, were analyzed by flow cytometry (n = 3/group). The ratio of CD8+ T cells to CD4+ T cells in the liver of trametinib-treated mice tended to be lower than that in the vehicle-treated group (Figure 4A; 1-way ANOVA; P = 0.26), indicating that trametinib suppresses infiltration of the liver by CD8+ T cells. Among the different CD4+ T-cell subpopulations, trametinib increased the percentage of naive T cells (CD62L+CD44–) in the liver in a dose-dependent manner; it also reduced the percentage of effector memory T cells (CD62L-CD44+) in the liver and spleen (Figure 4B; 1-way ANOVA; all P < 0.05). By contrast, trametinib had no effect on CD8+ T-cell subpopulations in the liver or spleen (Figure 4C). These results suggest that (at least in vivo) trametinib mainly suppresses functional differentiation of CD4+ naive T cells. Reference: Transplant Direct. 2020 Sep; 6(9): e591. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7423917/
Solvent mg/mL mM
Solubility
DMSO 27.7 44.96
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 615.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Itamura H, Shindo T, Tawara I, Kubota Y, Kariya R, Okada S, Komanduri KV, Kimura S. The MEK inhibitor trametinib separates murine graft-versus-host disease from graft-versus-tumor effects. JCI Insight. 2016 Jul 7;1(10):e86331. doi: 10.1172/jci.insight.86331. PMID: 27699218; PMCID: PMC5033881. 2. Bridgeman VL, Wan E, Foo S, Nathan MR, Welti JC, Frentzas S, Vermeulen PB, Preece N, Springer CJ, Powles T, Nathan PD, Larkin J, Gore M, Vasudev NS, Reynolds AR. Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma. Mol Cancer Ther. 2016 Jan;15(1):172-83. doi: 10.1158/1535-7163.MCT-15-0170. Epub 2015 Oct 20. PMID: 26487278. 3. Tada S, Anazawa T, Shindo T, Yamane K, Inoguchi K, Fujimoto N, Nagai K, Masui T, Okajima H, Takaori K, Sumi S, Uemoto S. The MEK Inhibitor Trametinib Suppresses Major Histocompatibility Antigen-mismatched Rejection Following Pancreatic Islet Transplantation. Transplant Direct. 2020 Aug 12;6(9):e591. doi: 10.1097/TXD.0000000000001045. PMID: 32851124; PMCID: PMC7423917. 4. Bridgeman VL, Wan E, Foo S, Nathan MR, Welti JC, Frentzas S, Vermeulen PB, Preece N, Springer CJ, Powles T, Nathan PD, Larkin J, Gore M, Vasudev NS, Reynolds AR. Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma. Mol Cancer Ther. 2016 Jan;15(1):172-83. doi: 10.1158/1535-7163.MCT-15-0170. Epub 2015 Oct 20. PMID: 26487278.
In vitro protocol:
1. Itamura H, Shindo T, Tawara I, Kubota Y, Kariya R, Okada S, Komanduri KV, Kimura S. The MEK inhibitor trametinib separates murine graft-versus-host disease from graft-versus-tumor effects. JCI Insight. 2016 Jul 7;1(10):e86331. doi: 10.1172/jci.insight.86331. PMID: 27699218; PMCID: PMC5033881. 2. Bridgeman VL, Wan E, Foo S, Nathan MR, Welti JC, Frentzas S, Vermeulen PB, Preece N, Springer CJ, Powles T, Nathan PD, Larkin J, Gore M, Vasudev NS, Reynolds AR. Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma. Mol Cancer Ther. 2016 Jan;15(1):172-83. doi: 10.1158/1535-7163.MCT-15-0170. Epub 2015 Oct 20. PMID: 26487278.
In vivo protocol:
1. Tada S, Anazawa T, Shindo T, Yamane K, Inoguchi K, Fujimoto N, Nagai K, Masui T, Okajima H, Takaori K, Sumi S, Uemoto S. The MEK Inhibitor Trametinib Suppresses Major Histocompatibility Antigen-mismatched Rejection Following Pancreatic Islet Transplantation. Transplant Direct. 2020 Aug 12;6(9):e591. doi: 10.1097/TXD.0000000000001045. PMID: 32851124; PMCID: PMC7423917. 2. Bridgeman VL, Wan E, Foo S, Nathan MR, Welti JC, Frentzas S, Vermeulen PB, Preece N, Springer CJ, Powles T, Nathan PD, Larkin J, Gore M, Vasudev NS, Reynolds AR. Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma. Mol Cancer Ther. 2016 Jan;15(1):172-83. doi: 10.1158/1535-7163.MCT-15-0170. Epub 2015 Oct 20. PMID: 26487278.
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Cytokine release syndrome induced by dabrafenib and trametinib therapy in BRAF V600E-mutant non- small cell lung cancer. Jpn J Clin Oncol. 2025 Jan 17:hyaf004. doi: 10.1093/jjco/hyaf004. Epub ahead of print. PMID: 39821273. 4: Liu H, Karsidag M, Chhatwal K, Wang P, Tang T. Single-cell and bulk RNA sequencing analysis reveals CENPA as a potential biomarker and therapeutic target in cancers. PLoS One. 2025 Jan 16;20(1):e0314745. doi: 10.1371/journal.pone.0314745. PMID: 39820192; PMCID: PMC11737691. 5: Zhang S, Deng S, Liu J, Liu S, Chen Z, Liu S, Xue C, Zeng L, Zhao H, Xu Z, Zhao S, Zhou Y, Peng X, Wu X, Bai R, Wu S, Li M, Zheng J, Lin D, Zhang J, Huang X. Targeting MXD1 sensitises pancreatic cancer to trametinib. Gut. 2025 Jan 16:gutjnl-2024-333408. doi: 10.1136/gutjnl-2024-333408. Epub ahead of print. PMID: 39819860. 6: Campochiaro C, Tomelleri A, Catamerò F, Pegoraro F, Vaglio A, Dagna L. Anakinra improves retention rate of targeted treatments in Erdheim-Chester disease. Rheumatology (Oxford). 2025 Jan 15:keaf023. doi: 10.1093/rheumatology/keaf023. Epub ahead of print. PMID: 39814074. 7: Yeh CN, Lin SF, Wu CL, Liou MJ, Chen IW, Chen CP, Chang CF, Wang QA, Wu CE. Genomic landscape and comparative analysis of tissue and liquid-based NGS in Taiwanese anaplastic thyroid carcinoma. NPJ Precis Oncol. 2025 Jan 14;9(1):16. doi: 10.1038/s41698-025-00802-2. PMID: 39809865; PMCID: PMC11733018. 8: Leng W, Wei G, Sheng L, Jiang D, Qiu M. E203K mutation in MAP2K1 (MEK1) causes acquired resistance to PD-1 blockade but responds to trametinib: a case report. Chin Clin Oncol. 2024 Dec;13(6):87. doi: 10.21037/cco-24-61. PMID: 39806853. 9: Wang Y, Li X, Wang Y, Qin J. Establishment and characterization of a new mouse gastric carcinoma cell line, MCC. Cancer Cell Int. 2025 Jan 12;25(1):9. doi: 10.1186/s12935-024-03633-6. PMID: 39800685; PMCID: PMC11727671. 10: Sait SF, Tang KH, Angus SP, Brown R, Sun D, Xie X, Iltis C, Lien M, D Socci N, Bale TA, Davis C, Dixon SAH, Zhang C, Wade Clapp D, Neel BG, Parada LF. Hydroxychloroquine prevents resistance and potentiates the antitumor effect of SHP2 inhibition in NF1-associated malignant peripheral nerve sheath tumors. Proc Natl Acad Sci U S A. 2025 Jan 7;122(1):e2407745121. doi: 10.1073/pnas.2407745121. Epub 2024 Dec 30. PMID: 39793045; PMCID: PMC11725864. 11: Zumwalt L, Schluterman H, Ray A, Heym K. Life-threatening Lymphatic Malformation With Somatic Activating NRAS Mutation Successfully Treated With Trametinib: A Case Study. J Pediatr Hematol Oncol. 2025 Jan 3. doi: 10.1097/MPH.0000000000002990. Epub ahead of print. PMID: 39792794. 12: Ye L, Long C, Xu B, Yao X, Yu J, Luo Y, Xu Y, Jiang Z, Nian Z, Zheng Y, Cai Y, Xue X, Guo G. Multi‑omics identification of a novel signature for serous ovarian carcinoma in the context of 3P medicine and based on twelve programmed cell death patterns: a multi-cohort machine learning study. Mol Med. 2025 Jan 8;31(1):5. doi: 10.1186/s10020-024-01036-x. PMID: 39773329; PMCID: PMC11707953. 13: Proietti I, Azzella G, Dirzu D, Di Cristofano C, Bagni O, Potenza C, Filippi L. It Looks Like a Zebra but Is Not: [18F]FDG PET/CT in a Giant Cutaneous Malignant Melanoma Mimicking Squamous Cell Carcinoma. Diagnostics (Basel). 2024 Dec 19;14(24):2860. doi: 10.3390/diagnostics14242860. PMID: 39767221; PMCID: PMC11675548. 14: Suzuki M, Koga Y, Kawasaki T, Ueda T, Yamamoto S, Goto H, Kishimoto J, Ishida E, Todaka K, Sonoda KH, Oda Y, Koji Y, Sakai Y, Ohga S. Access Program for Unapproved and Off-Label Drug Use in Pediatric BRAF V600E-Mutated Brain Tumors in Japan. Pediatr Blood Cancer. 2025 Jan 6:e31510. doi: 10.1002/pbc.31510. Epub ahead of print. PMID: 39762715. 15: Anai S, Isa K, Chibana R, Ueno S, Sato Y. Remarkable Response to Dabrafenib and Trametinib in a V-Raf Murine Sarcoma Viral Oncogene Homolog B (BRAF) V600E-Mutated Lung Adenocarcinoma Patient With Poor Performance Status and Respiratory Failure: A Case Report. Cureus. 2024 Dec 6;16(12):e75217. doi: 10.7759/cureus.75217. PMID: 39759653; PMCID: PMC11700529. 16: Dhatt J, Houser K, Szymanski KA, Halderman K, Kuwabara M. Wyburn-Mason disease: Management of a Spetzler-Martin grade 5 arteriovenous malformation with predominant thalamic involvement. Radiol Case Rep. 2024 Dec 12;20(3):1323-1327. doi: 10.1016/j.radcr.2024.11.023. PMID: 39758327; PMCID: PMC11700262. 17: Kato AS, Shwaish NS, Hwang EY, Mandapati R, Lee JW. Novel use of trametinib for treatment of atrial arrhythmia in absence of cardiomyopathy in a patient with Costello syndrome. Cardiol Young. 2025 Jan 6:1-3. doi: 10.1017/S1047951124036126. Epub ahead of print. 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