Tomivosertib, also known as eFT508 is a MNK1/2 inhibitor. Tomivosertib binds to and inhibits the activity of MNK1 and 2. This prevents MNK1/2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling.
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Name | Tomivosertib HCl |
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Iupac Chemical Name | 6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione hydrochloride |
Synonyms | Tomivosertib HCl; hydrochloride; Tomivosertib HCl; eFT508; eFT-508; eFT 508; eFT508 hydrochloride |
Molecular Formula | C17H21ClN6O2 |
Molecular Weight | 376.84 |
Smile | O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4.[H]Cl |
InChiKey | WBGPPUUXCGKTSC-UHFFFAOYSA-N |
InChi | InChI=1S/C17H20N6O2.ClH/c1-10-7-11(21-13-8-12(18)19-9-20-13)16(25)23-14(10)15(24)22-17(23)5-3-2-4-6-17;/h7-9H,2-6H2,1H3,(H,22,24)(H3,18,19,20,21);1H |
CAS Number | 1849590-02-8 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | Refer to MSDS |
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. |
HS Code | 2934200090 |
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Mechanism | |
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1: Megat S, Ray PR, Moy JK, Lou TF, Barragan-Iglesias P, Li Y, Pradhan G,
Wanghzou A, Ahmad A, Burton MD, North RY, Dougherty PM, Khoutorsky A, Sonenberg
N, Webster KR, Dussor G, Campbell ZT, Price TJ. Nociceptor translational
profiling reveals the Ragulator-Rag GTPase complex as a critical generator of
neuropathic pain. J Neurosci. 2018 Nov 20. pii: 2661-18. doi:
10.1523/JNEUROSCI.2661-18.2018. [Epub ahead of print] PubMed PMID: 30459229.
2: Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B,
Ernst JT, Han Q, Goel VK, Han EZR, Huang V, Hung INJ, Jemison A, Jessen KA,
Molter J, Murphy D, Neal M, Parker GS, Shaghafi M, Sperry S, Staunton J, Stumpf
CR, Thompson PA, Tran C, Webber SE, Wegerski CJ, Zheng H, Webster KR.
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated
Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1
and 2 (MNK1/2) Inhibition. J Med Chem. 2018 Apr 26;61(8):3516-3540. doi:
10.1021/acs.jmedchem.7b01795. Epub 2018 Mar 29. PubMed PMID: 29526098.
3: Dreas A, Mikulski M, Milik M, Fabritius CH, Brzózka K, Rzymski T.
Mitogen-activated Protein Kinase (MAPK) Interacting Kinases 1 and 2 (MNK1 and
MNK2) as Targets for Cancer Therapy: Recent Progress in the Development of MNK
Inhibitors. Curr Med Chem. 2017;24(28):3025-3053. doi:
10.2174/0929867324666170203123427. Review. PubMed PMID: 28164761.