SJF 0628

Name: SJF 0628
Brand: Tocris Bioscience
SKU: 7463
Price: 321 USD

Tocris Bioscience a Bio-Techne Brand

Catalog # 7463

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Key Product Details

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)
Molecular Weight:	1010.19

View Full Technical Details for SJF 0628

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 BRAF^WT protein. The product degrades mutant BRAF^V600E 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 for SJF 0628

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	9.90 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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References for SJF 0628

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

Alabi Mutant-selective degradation by BRAF-targeting PROTACs. Nat.Commun. 2021 PMID: 33568647

Citations for SJF 0628

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