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MS 28

Cat. No. 8076 Submit a Review Datasheet / COA / SDS
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Description: Cyclin D1, CDK4/6 and cyclin D3 Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(7-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 28

MS 28 is a cyclinD1 Degrader (PROTAC®) (DC50 = 950 nM; Dmax = 90% in vitro). Also degrades CDK4, CDK6 and cyclin D3 after 4 hours. Degrades cyclin D1 and cyclin D3 by recruiting the CDK4/6 as a 'bridge'. Comprises a CDK4/6 binding moiety joined by a linker to a VHL ligand. Suppresses NCI-H2110 and Calu-1 cancer cell growth at 1 μM.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Technical Data for MS 28

M. Wt 1002.25
Formula C53H67N11O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2229974-73-4
PubChem ID 146014438
InChI Key MWVNDEBEHBRZEC-WWTLGBROSA-N
Smiles O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N5CCN(CC5)C(CCCCCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)=O)=O)C=N4)=NC=C3C(C)=C1C(C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MS 28

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.22 100

Preparing Stock Solutions for MS 28

The following data is based on the product molecular weight 1002.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1 mL 4.99 mL 9.98 mL
5 mM 0.2 mL 1 mL 2 mL
10 mM 0.1 mL 0.5 mL 1 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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References for MS 28

References are publications that support the biological activity of the product.

Xiong et al (2022) Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets. J.Am.Chem.Soc. 144 22622 PMID: 36448571

If you know of a relevant reference for MS 28, please let us know.

View Related Products by Target

Keywords: MS 28, MS 28 supplier, MS28, degrader, degrades, degraders, protac, proteolysis, chimera, cdk, cdk4, cdk6, cyclin, cyclind1, cyclind3, bridge, VHL, von, hippel, lindau, E3, ligase, Cyclin, Dependent, Kinase, (CDK), Degraders, 8076, Tocris Bioscience

Citations for MS 28

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia