SJFα

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Cat.No. 7268 - SJFaSJFalphaSJFalpha | C59H67F2N7O11S | CAS No. 2254609-27-1
Description: Potent and selective p38α PROTAC®
Alternative Names: SJFa PROTAC, SJFalpha PROTAC, SJFα PROTAC
Chemical Name: N-(3-Fluoro-4-((7-(4-(4-(2-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)butoxy)butoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Potent and selective p38α PROTAC® Degrader (DC50 = 7.16 nM and Dmax = 97.4%). SJFα comprises the multikinase inhibitor foretinib joined by a linker to a VHL ligand. Displays significantly lower potency degradation at p38δ (DC50 = 299 nM). Exhibits no significant degradation of p38β or γ. or related MAPKs, ERK1/2, or JNK1/2.

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

Technical Data

M. Wt 1120.28
Formula C59H67F2N7O11S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2254609-27-1
PubChem ID 137628677
InChI Key GXDYWQXTEYENEU-WFYKIECOSA-N
Smiles COC1=CC2=C(N=CC=C2OC3=C(C=C(C=C3)NC(C4(C(NC5=CC=C(C=C5)F)=O)CC4)=O)F)C=C1OCCCCOCCCCOCC(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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 112.03 100

Preparing Stock Solutions

The following data is based on the product molecular weight 1120.28. 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 0.89 mL 4.46 mL 8.93 mL
5 mM 0.18 mL 0.89 mL 1.79 mL
10 mM 0.09 mL 0.45 mL 0.89 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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References

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

Smith et al (2019) Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase. Nat. Commun. 10 131 PMID: 30631068


If you know of a relevant reference for SJFα, please let us know.

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Citations for SJFα

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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!

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Epigenetics

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

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, 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

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