Tomivosertib (eFT508)

製品コードS8275 バッチS827501

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₂₀N₆O₂
	分子量	340.38	CAS No.	1849590-01-7
Solubility (25°C)*	体外	DMSO	13 mg/mL (38.19 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
in vitro	Tomivosertib (eFT-508) 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 this compound leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, this chemical shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to this compound 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.
in vivo	Tomivosertib (eFT-508) is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of this compound is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	TMD8 cells
	濃度	0.01, 0.1, 1, 3, 10 μM
	反応時間	24 h
	実験の流れ	TMD8 cells are treated with the indicated concentrations of Tomivosertib (eFT-508) for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies.
動物実験	動物モデル	TMD8 xenograft bearing animals
	投薬量	1 mg/kg or 10 mg/kg
	投与方法	p.o.

参考

http://effector.com/wp-content/uploads/2015/12/eFFECTOR-ASH-2015-poster_final.pdf

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Prolonging lung cancer response to EGFR inhibition by targeting the selective advantage of resistant cells [ Nat Commun, 2025, 16(1):7853]	PubMed: 40846697
Increased translation driven by non-canonical EZH2 creates a synthetic vulnerability in enzalutamide-resistant prostate cancer [ Nat Commun, 2024, 15(1):9755]	PubMed: 39567499
MNK-driven eIF4E phosphorylation regulates the fibrogenic transformation of mesenchymal cells and chronic lung allograft dysfunction [ J Clin Invest, 2024, 134(16)e168393]	PubMed: 39145446
Blocking tumor-intrinsic MNK1 kinase restricts metabolic adaptation and diminishes liver metastasis [ Sci Adv, 2024, 10(37):eadi7673]	PubMed: 39270021
TSC2 loss in neural progenitor cells suppresses translation of ASD/NDD-associated transcripts in an mTORC1- and MNK1/2-reversible fashion [ bioRxiv, 2024, 2024.06.04.597393]	PubMed: 38895292
Cooperative activation of PDK1 and AKT by MAPK4 enhances cancer growth and resistance to therapy [ PLoS Biol, 2023, 21(8):e3002227]	PubMed: 37531320
MAPK-interacting kinases inhibition by eFT508 overcomes chemoresistance in preclinical model of osteosarcoma [ Hum Exp Toxicol, 2023, 42:9603271231158047]	PubMed: 36840478
Prolonging lung cancer response to EGFR inhibition by targeting the selective advantage of resistant cells [ BioRxiv, 2023, 10.1101/2023.06.19.545595]	PubMed: none
Culture media composition influences patient-derived organoid ability to predict therapeutic responses in gastrointestinal cancers [ JCI Insight, 2022, 7(22e158060)]	PubMed: 36256477
Treatment with eFT-508 increases chemosensitivity in breast cancer cells by modulating the tumor microenvironment [ J Transl Med, 2022, 20(1):276]	PubMed: 35717238

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。