SJ 1008030

Name: SJ 1008030
Brand: Tocris Bioscience
SKU: 7675

Tocris Bioscience, part of Bio-Techne | Catalog # 7675

COA / SDS

Selective JAK2 Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	987.97

View Full Technical Details for SJ 1008030

Technical Data
Citations

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 for SJ 1008030

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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	0.40 mL	2.02 mL	4.05 mL
5 mM	0.20 mL	1.01 mL	2.02 mL
25 mM	0.04 mL	0.20 mL	0.40 mL

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References for SJ 1008030

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

Constantinescu Degrading JAK2 in ALL by ruxolitinib-based PROTACs. Blood 2021 PMID: 34882211
Chang Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood 2021 PMID: 34110416