Tomivosertib

SKU: orb1304174

Description

Tomivosertib (eFT508) is a highly selective, potent dual inhibitor of MNK1 and MNK2 kinases, exhibiting IC50 values in the low nanomolar range. It is widely used in preclinical research to investigate MNK's role in oncogenesis and immune modulation, demonstrating antitumor activity in both cellular assays and in vivo animal models.

Research Area

Cell Biology, Immunology & Inflammation, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1849590-01-7
MW	340.38
Purity	99.72% (May vary between batches)
Formula	C₁₇H₂₀N₆O₂
SMILES	Cc1cc(Nc2cc(N)ncn2)c(=O)n2c1C(=O)NC21CCCCC1
Target	MNK,PD-1/PD-L1
Solubility	H2O:<1 mg/mL;DMSO:11 mg/mL (32.32 mM);Ethanol:<1 mg/mL

Bioactivity

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Target IC50	MNK2:1-2 nM\|MNK1:1-2 nM
In Vivo	eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations. Read more...
In Vitro	Tomivosertib has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with Tomivosertib leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10. Read more...
Cell Research	TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies. (Only for Reference) Read more...

Storage & Handling

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Storage	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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PD-L1, PDL1, Tomivosertib, PD-1/PD-L1, PD1/PDL1, PD1, PD-1, Mitogen activated protein kinase interacting kinase, MNK, MNK1, MNK2, Inhibitor, inhibit, MAP kinase interacting kinase, MAPK interacting kinase, eFT 508, eFT508, eFT-508

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Compound Identifiers

PubChem CID

118598754 ↗

Key Properties

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No computed properties available.

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Tomivosertib (orb1304174)

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CAS Number:	1849590-02-8
MW:	376.845
Formula:	C₁₇H₂₁ClN₆O₂

Purity:	>98% (HPLC)
CAS Number:	1849590-01-7
MW:	340.3797
Formula:	C₁₇H₂₀N₆O₂

Tomivosertib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Tomivosertib HCl [orb1739356]

eFT508 [orb1225854]

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