[CAS NO. 1849590-01-7] Tomivosertib

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PRODUCTS SPECIFICATIONS [1849590-01-7]

Catalog

HY-100022

Brand

MCE

CAS

1849590-01-7

DESCRIPTION [1849590-01-7]

Overview

MDL	MFCD30489732
Molecular Weight	340.38
Molecular Formula	C17H20N6O2
SMILES	O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC ₅₀ s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC ₅₀ =2-16 nM) in tumor cell lines ^[1] . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance ^[2] .

IC50 & Target

MNK1

1-2 nM (IC ₅₀ )

MNK2

1-2 nM (IC ₅₀ )

PD-L1

In Vitro

Tomivosertib (eFT508) reduces eIF4E phosphorylation dose-dependently at serine 209 (IC ₅₀ =2-16 nM) in tumor cell lines. In a panel of appr 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. Further evaluation Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04261218	Translational Research in Oncology\|Effector Therapeutics\|Stand Up To Cancer	Breast Cancer	August 25, 2020	Phase 1
NCT04622007	Effector Therapeutics\|Medpace, Inc.	Non-small Cell Lung Cancer	June 2, 2021	Phase 2
NCT02937675	Effector Therapeutics	Lymphoma	February 8, 2017	Phase 1\|Phase 2
NCT02605083	Effector Therapeutics	Cancer	December 3, 2015	Phase 1\|Phase 2
NCT03690141	Effector Therapeutics	Castrate-resistant Prostate Cancer (CRPC)	October 12, 2018	Phase 2
NCT03318562	Effector Therapeutics	Triple Negative Breast Cancer\|Hepatocellular Carcinoma	November 21, 2017	Phase 2
NCT03258398	Effector Therapeutics\|Merck KGaA, Darmstadt, Germany\|Pfizer	Microsatellite Stable Relapsed or Refractory Colorectal Cancer	September 18, 2017	Phase 2
NCT03616834	Effector Therapeutics	Solid Tumors	July 25, 2018	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 4.35 mg/mL ( 12.78 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9379 mL	14.6895 mL	29.3789 mL
5 mM	0.5876 mL	2.9379 mL	5.8758 mL
10 mM	0.2938 mL	1.4689 mL	2.9379 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.44 mg/mL (1.29 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.43 mg/mL (1.26 mM); Clear solution
3.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic
4.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.