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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)
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) also available.
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 |
| InChI Key | MBCAVOCJJAQHHT-FGUOTCRGSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for SJF 0628
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.
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Keywords: SJF 0628, SJF 0628 supplier, SJF0628, BRAFV600E, kinase, inhibitors, degraders, PROTAC, degradation, raf, high, affinity, potent, Raf, Kinase, Active, Degraders, 7463, Tocris Bioscience
Citations for SJF 0628
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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
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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 PosterUpdated
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
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