SJF 0628

Tocris Bioscience | Catalog # 7463

Potent BRAF Degrader (PROTAC®
Tocris Bioscience

Key Product Details

Description

Potent BRAF Degrader (PROTAC®
View all Active Degraders »

Product Description

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.

Product Specifications for SJF 0628

Molecular Weight

1010.19

Formula

C51H57F2N9O7S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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 all 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 9.90 mL
5 mM 0.20 mL 0.99 mL 1.98 mL
10 mM 0.10 mL 0.49 mL 0.99 mL
50 mM 0.02 mL 0.10 mL 0.20 mL

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Background References

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

Product Documents for SJF 0628

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for SJF 0628

For research use only

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