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说明： Selective JAK2 Degrader (PROTAC®)
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
许可信息
Sold under license from St. Jude Children's Research Hospital
技术数据 for SJ 1008030
| 分子量 | 987.97 |
| 公式 | C42H43N13O7S.CF3CO2H |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SJ 1008030
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 49.4 | 50 |
制备储备液 for SJ 1008030
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SJ 1008030
参考文献 for SJ 1008030
参考文献是支持产品生物活性的出版物。
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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TPD and Induced Proximity Research Product GuideUpdated
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
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