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CS-2450

EFT-508

CAS: 1849590-01-7

Molecular Formula: C17H20N6O2

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CS-2450 - Names and Identifiers

Name EFT-508
Synonyms EFT-508
CS-2450
eFT-508
eFT508 -MNK
Tomivosertib
eFT-508 (eFT508)
Tomivosertib eFT508
6'-[(6-Amino-4-pyrimidinyl)amino]-8'-methylspiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione
6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione
CAS 1849590-01-7

CS-2450 - Physico-chemical Properties

Molecular FormulaC17H20N6O2
Molar Mass340.3797
Density1.43±0.1 g/cm3(Predicted)
Melting Point>300°C
Boling Point735.6±60.0 °C(Predicted)
Solubility DMSO: 6 mg/mL (Need ultrasonic)
AppearanceForm Solid, color Pale Yellow
pKa13.77±0.60(Predicted)
Storage ConditionRefrigerator, under inert atmosphere
Physical and Chemical PropertiesBioactive Tomivosertib (eFT-508) is an effective and selective inhibitor of MNK1/2 with IC50 of 2.4 nM and 1 nM respectively. It can reduce the proliferation of tumor cells and tumor growth. Tomivosertib (eFT-508) inhibited eIF4E phosphorylation and significantly down-regulated PD-L1 protein abundance.

CS-2450 - Preparation solution concentration reference

 1mg5mg10mg
1 mM2.938 ml14.689 ml29.379 ml
5 mM0.588 ml2.938 ml5.876 ml
10 mM0.294 ml1.469 ml2.938 ml
5 mM0.059 ml0.294 ml0.588 ml
Last Update:2024-01-02 23:10:35

CS-2450 - Nature

Solubility DMSO (Slightly, Heated), Methanol (Very Slightly)
Last Update:2024-04-10 22:29:15

CS-2450 - Uses and synthesis methods

Target

Target Value

MNK2

(Cell-free assay) 1 nM

MNK1

(Cell-free assay) 2.4 nM

in vitro studies

In enzymatic experiments, the IC50 values of eFT508 for MNK1/2L subtypes are in the range of 1-2 nM, and the inhibition of MNK is a reversible and ATP competitive process. Treatment of cancer cell lines with eFT508 will result in a concentration-dependent decrease in intracellular eIF4E phosphorylation of serine at position 209, with IC50 = 2-16 nM. Among ~ 50 hematological tumors, eFT508 has antiproliferative activity against multiple DLBCL cell lines. The sensitivity of TMD8, OCL-Ly3 and HBL1 DLBCL cells to eFT508 is related to the concentration-dependent decrease of pro-inflammatory factors (such as TNFα, IL-6, IL-10 and CXCL10).

In vivo studies

eFT508 is well tolerated in vivo and is very effective in MyD88-mutant DLBCL models. In TMD8 and HBL-1 ABC-DLBCL models (subcutaneous injection of human lymphoma xenograft model),eFT508 has significant anti-tumor activity.

Last Update:2024-04-09 21:01:54
CS-2450
Supplier List
Shanghai Macklin Biochemical Co., Ltd
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CAS: 1849590-01-7
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Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: eFT-508 (eFT508) Visit Supplier Webpage Request for quotation
CAS: 1849590-01-7
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: eFT508 Request for quotation
CAS: 1849590-01-7
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: eFT508 Visit Supplier Webpage Request for quotation
CAS: 1849590-01-7
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: eFT508 Visit Supplier Webpage Request for quotation
CAS: 1849590-01-7
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
BOC Sciences
Spot supply
Product Name: eFT-508 Visit Supplier Webpage Request for quotation
CAS: 1849590-01-7
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: eFT508 Visit Supplier Webpage Request for quotation
CAS: 1849590-01-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
CS-2450
NSC 4754
黄蝶呤
6331-09-5
2-chloro-6-fluorophenylethanol
5853-29-2
1786-08-9
23915-08-4
88-69-7
6836-22-2
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