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MS4078

Catalog No. T16153   CAS 2229036-62-6

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

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MS4078 Chemical Structure
MS4078, CAS 2229036-62-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
2 mg In stock $ 64.00
5 mg In stock $ 97.00
10 mg In stock $ 163.00
25 mg In stock $ 289.00
50 mg In stock $ 463.00
100 mg In stock $ 683.00
1 mL * 10 mM (in DMSO) In stock $ 163.00
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Purity: 98.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.
Targets&IC50 NPM-ALK:11 nM(DC50)(SU-DHL-1 cells), ALK:33 nM(SU-DHL-1 cells), EML4-ALK:59 nM(DC50)(NCI-H2228 cells)
In vitro MS4078 effectively inhibits cancer cell proliferation. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1?cells with IC50 of 33 nM. MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228?cells in a concentration-dependent manner. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively.
Molecular Weight 914.47
Formula C45H52ClN9O8S
CAS No. 2229036-62-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49 mg/mL (53.58 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Angiogenesis related Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library Hematonosis Compound Library Anti-Cancer Compound Library

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Keywords

MS4078 2229036-62-6 Angiogenesis PROTAC Tyrosine Kinase/Adaptors ALK Ligand for E3 Ligase Anaplastic lymphoma kinase CD246 Inhibitor MS 4078 ALK tyrosine kinase receptor inhibit MS-4078 Anaplastic lymphoma kinase (ALK) PROTACs Cluster of differentiation 246 inhibitor

 

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