SJF 0628

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Cat.No. 7463 - SJF 0628 | C51H57F2N9O7S2 | CAS No. 2413035-41-1
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)
Datasheet
Citations
Reviews
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) 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.

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, Active, Degraders, 7463, Tocris Bioscience

Citations for SJF 0628

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Literature in this Area

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