SJ10542
Based on 1 Customer Validation
SJ10542 is a potent and selective JAK2/3 PROTAC degrader, with DC50 values of 14 nM and 11 nM against JAK2 and JAK3, respectively. SJ10542 exhibits anti-tumor activity and can be used for research on acute lymphoblastic leukemia.
(Pink: JAK2 and JAK3 Target protein ligand; Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W251248)).
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- Purity: 99.32%
- CAS No.: 2789678-92-6
- 화학식: C41H46N12O5S
- 분자량:818.95
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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JAK2 14 nM (DC50) |
JAK3 11 nM (DC50) |
Cereblon 20 pM (IC50) |
JAK2 22 pM (IC50) |
SJ10542 (1-9000 nM; 24 h) potently degrades JAK2 (DC50 = 14 nM) and JAK3 (DC50 = 11 nM) in PDX SJBALL020589 cells, while exerts no significant degradation effect on JAK1, TYK2 or GSPT1[1].
SJ10542 (1-9000 nM; 24 h) efficiently and selectively degrades JAK2 in a CRBN-dependent manner in MHH-CALL-4 and KOPN49 cells, with DC50 values of 24 nM and 74 nM, respectively, while exerting no significant degradation effect on JAK1, TYK2 or GSPT1[1].
SJ10542 (0.1-10000 nM) exhibits potent cytotoxicity against PDX SJBALL020589 cells (IC50 = 24 nM)[1].
SJ10542 exhibits cytotoxic activity (IC50 < 120 nM)[1] in all tested JAK-STAT-driven PDX acute lymphoblastic leukemia models.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:patient-derived acute lymphoblastic leukemia (PDX) cells SJBALL020589 (harboring ATF7IP-JAK2 fusion, KMT2C R3382W, PIK3CD F146I)
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Concentration:1, 10, 100, 1000 and 9000 nM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of both JAK2 and JAK3, with a DC50 of 14 nM (Dmax 90%) for JAK2 and a DC50 of 11 nM (Dmax 92%) for JAK3.
Left JAK1, TYK2, and GSPT1 protein levels largely unaffected.
Chemical Information
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CAS No. 2789678-92-6
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Appearance Solid
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분자량 818.95
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화학식 C41H46N12O5S
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Color White to off-white
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SMILES
O=C(C1=CC=C(NC2=NC(NC=C3)=C3C(C4=CN(C5(CN(S(=O)(CC)=O)C5)CC#N)N=C4)=N2)C=C1)NCCCN(CC6)CCN6C7=CC=C(C=C7)C8C(NC(CC8)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 46.67 mg/mL (56.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2211 mL | 6.1054 mL | 12.2108 mL | 30.5269 mL |
| 5 mM | 0.2442 mL | 1.2211 mL | 2.4422 mL | 6.1054 mL | |
| 10 mM | 0.1221 mL | 0.6105 mL | 1.2211 mL | 3.0527 mL | |
| 15 mM | 0.0814 mL | 0.4070 mL | 0.8141 mL | 2.0351 mL | |
| 20 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 25 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2211 mL | |
| 30 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0176 mL | |
| 40 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7632 mL | |
| 50 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 mL |
SJ10542 Related Classifications
HY-145696 Related Classifications
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