CST 905

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Description: Potent and selective BRAFV600E Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(2-(4-(4-(3-(3-((N-Ethyl-N-methylsulfamoyl)amino)-2,6-difluorobenzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for CST 905

CST 905 is a potent and selective BRAFV600E Degrader (PROTAC®) (DC50 = 18 nM). CST 905 comprises a ligand for the von Hippel Lindau (VHL) E3 ligase joined by a linker to a PLX-derived ligand. Unlike other BRAFV600E Degraders, CST 905 does not activate ERK.

B-Raf antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3424.

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

Technical Data for CST 905

M. Wt 1025.2
Formula C51H58F2N10O7S2
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key VOFGLMSAVUMRLF-FGUOTCRGSA-N
Smiles FC1=C(C(F)=CC=C1NS(N(C)CC)(=O)=O)C(C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)N5CCN(CC5)CC(N[C@H](C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)C(C)(C)C)=O)=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 CST 905

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 102.52 100

Preparing Stock Solutions for CST 905

The following data is based on the product molecular weight 1025.2. 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 0.98 mL 4.88 mL 9.75 mL
5 mM 0.2 mL 0.98 mL 1.95 mL
10 mM 0.1 mL 0.49 mL 0.98 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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References for CST 905

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

Miller et al (2022) Encoding BRAF inhibitor functions in protein degraders. RSC Med.Chem. 13 731 PMID: 35814929


If you know of a relevant reference for CST 905, please let us know.

Keywords: CST 905, CST 905 supplier, CST905, degraders, degradation, targeted, protein, degrader, E3, ligase, protac, BRAF, V600E, BRAFV600E, potent, selective, VHL, von, hippel, lindau, PLX, ERK, Protein, Degraders, Raf, Kinase, 7745, Tocris Bioscience

Citations for CST 905

Citations are publications that use Tocris products.

Currently there are no citations for CST 905. Do you know of a great paper that uses CST 905 from Tocris? Please let us know.

Reviews for CST 905

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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