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BSJ-04-132

Cat. No. 6937 Submit a Review Datasheet / COA / SDS
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Description: Selective Cdk4 Degrader (PROTAC®)
Chemical Name: 7-Cyclopentyl-2-[[5-[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl]oxy]acetamido]butyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethyl-7H-pyrrolo[2,3d]pyrimidine-6-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for BSJ-04-132

BSJ-04-132 is a selective Cdk4 Degrader (PROTAC®). Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation.

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

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for BSJ-04-132

M. Wt 819.92
Formula C42H49N11O7
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2349356-39-2
InChI Key GWLSXEHHNOBFOI-UHFFFAOYSA-N
Smiles O=C(COC1=C2C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)=CC=C1)NCCCCN4CCN(CC4)C5=CC=C(N=C5)NC6=NC7=C(C=C(C(N(C)C)=O)N7C8CCCC8)C=N6

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 BSJ-04-132

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 81.99 100

Preparing Stock Solutions for BSJ-04-132

The following data is based on the product molecular weight 819.92. 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 1.22 mL 6.1 mL 12.2 mL
5 mM 0.24 mL 1.22 mL 2.44 mL
10 mM 0.12 mL 0.61 mL 1.22 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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References for BSJ-04-132

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

Jiang et al (2019) Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angew.Chem.Int.Ed.Engl. 58 6321 PMID: 30802347

If you know of a relevant reference for BSJ-04-132, please let us know.

View Related Products by Target

Keywords: BSJ-04-132, BSJ-04-132 supplier, cyclin, dependent, kinase, cdk4, active, degraders, degrades, selective, protac, PROTACs, proteolysis, targeting, chimera, Active, Degraders, Cyclin-dependent, Kinase, CDK4, Subfamily, 6937, Tocris Bioscience

Citations for BSJ-04-132

Citations are publications that use Tocris products.

Currently there are no citations for BSJ-04-132. Do you know of a great paper that uses BSJ-04-132 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

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