SJF 1528

Name: SJF 1528
Brand: Tocris Bioscience
SKU: 7262

Tocris Bioscience, part of Bio-Techne | Catalog # 7262

COA / SDS

Potent EGFR PROTAC® Degrader; also degrades HER2

Key Product Details

Description:	Potent EGFR PROTAC^® Degrader; also degrades HER2
Chemical Name:	(2S,4R)-1-((S)-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6- yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	1030.61

View Full Technical Details for SJF 1528

Technical Data
Citations

Biological Activity for SJF 1528

SJF 1528 is a potent EGFR PROTAC^® Degrader (DC₅₀ values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. SJF 1528 comprises the EGFR inhibitor Lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC₅₀ = 102 nM for SKBr3 cells).

EGFR antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF231

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for SJF 1528

M. Wt	1030.61
Formula	C₅₅H₅₇ClFN₇O₈S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2230821-38-0
PubChem ID	135157151
InChi Key	ZSCOIFSUFMYZEZ-YSWDPXALSA-N
Smiles	CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCOCCOC4=CC=C(C5=CC6=C(N=CN=C6NC7=CC(Cl)=C(C=C7)OCC8=CC(F)=CC=C8)C=C5)C=C4)=O)=O)O)=O)SC=N1

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 1528

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	103.06	100

Preparing Stock Solutions for SJF 1528

The following data is based on the product molecular weight 1030.61.

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	0.97 mL	4.85 mL	9.70 mL
5 mM	0.19 mL	0.97 mL	1.94 mL
10 mM	0.10 mL	0.49 mL	0.97 mL
50 mM	0.02 mL	0.10 mL	0.19 mL

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References for SJF 1528

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

Burslem The advantages of targeted protein degradation over inhibition: An RTK case study. Cell Chem.Biol. 2018 PMID: 29129716