SJF 0628

Pricing Availability   Qty
Description: Potent BRAF PROTAC®
Chemical Name: (2S,4R)-1-((S)-2-(2-(4-(4-(3-(2,6-Difluoro-3-(propylsulfonamido)benzoyl)-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)
Literature (4)

Biological Activity for SJF 0628

SJF 0628 is a potent, high affinity and mutant-selective Degrader (PROTAC®) of BRAF, comprising a ligand for the von Hippel Lindau E3 ligase joined by a piperazine linker to the BRAF kinase inhibitor vemurafenib. SJF 0628 induces degradation of all 3 classes of BRAF mutant in BRAF-dependent cancer cells without inducing degradation of the BRAFWT protein. The product degrades mutant BRAFV600E in BRAF-driven cancer cell lines (DC50 = 6.8 nM - 28 nM). SJ 0628 inhibits phosphorylation of MEK and ERK in SK-MEL-28 cells (DC50 = 10 nM) and inhibits cell growth in mutant-BRAF driven cancer cells (EC50 = 37 nM).

SJF 0661 negative control (Cat. No. 7464) and 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 SJF 0628

M. Wt 1010.19
Formula C51H57F2N9O7S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2413035-41-1
PubChem ID 146547699
Smiles CCCS(=O)(NC1=CC=C(C(C(C2=CNC3=NC=C(C4=CC=C(N5CCN(CC5)CC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)O)=O)=O)C=C4)C=C23)=O)=C1F)F)=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 SJF 0628

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 101.02 100

Preparing Stock Solutions for SJF 0628

The following data is based on the product molecular weight 1010.19. 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 0.99 mL 4.95 mL 9.9 mL
5 mM 0.2 mL 0.99 mL 1.98 mL
10 mM 0.1 mL 0.49 mL 0.99 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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References for SJF 0628

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

Alabi et al (2021) Mutant-selective degradation by BRAF-targeting PROTACs. Nat.Commun. 12 PMID: 33568647

If you know of a relevant reference for SJF 0628, please let us know.

Keywords: SJF 0628, SJF 0628 supplier, SJF0628, BRAFV600E, kinase, inhibitors, degraders, PROTAC, degradation, raf, high, affinity, potent, Raf, Kinase, Protein, Degraders, 7463, Tocris Bioscience

Citations for SJF 0628

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Currently there are no citations for SJF 0628. Do you know of a great paper that uses SJF 0628 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!

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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