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SJ 1008030

Cat. No. 7675 Submit a Review Datasheet / COA / SDS
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Description: Selective JAK2 Degrader (PROTAC®)
Chemical Name: 4-((4-(1-(3-(Cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(2-(4-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)ethyl)benzamide trifluoroacetate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for SJ 1008030

SJ 1008030 is a potent and selective JAK2 Degrader (PROTAC®). This compound shows potent antileukemic efficacy in CRLF2r ALL (Acute Lymphoblastic Leukemia) cell lines (EC50 = 5.4 nM). SJ 1008030 induces dose-dependent JAK2 degradation (IC50 = 32 nM) in xenograft models of kinase-driven ALL, with no effect on GSPT1 levels.

JAK2 antibodies validated for Western Blot also available: Catalog # NBP2-59451 and AF2988.

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

Licensing Information

Sold under license from St. Jude Children's Research Hospital

Technical Data for SJ 1008030

M. Wt 987.97
Formula C42H43N13O7S.CF3CO2H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2863634-97-1
InChI Key RRJQTSMHAOAMTD-UHFFFAOYSA-N
Smiles CCS(=O)(N1CC(C1)(N2C=C(C3=C4C=CNC4=NC(NC5=CC=C(C(NCCN6CCN(C7=CC=C8C(N(C(C8=C7)=O)C9CCC(NC9=O)=O)=O)CC6)=O)C=C5)=N3)C=N2)CC#N)=O.OC(C(F)(F)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 SJ 1008030

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.4 50

Preparing Stock Solutions for SJ 1008030

The following data is based on the product molecular weight 987.97. 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
0.5 mM 2.02 mL 10.12 mL 20.24 mL
2.5 mM 0.4 mL 2.02 mL 4.05 mL
5 mM 0.2 mL 1.01 mL 2.02 mL
25 mM 0.04 mL 0.2 mL 0.4 mL

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References for SJ 1008030

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

Chang et al (2021) Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood 138 2313 PMID: 34110416

Constantinescu et al (2021) Degrading JAK2 in ALL by ruxolitinib-based PROTACs. Blood 138 2301 PMID: 34882211

If you know of a relevant reference for SJ 1008030, please let us know.

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Citations for SJ 1008030

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

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