SJ988497
Based on 1 Customer Validation
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL).
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- Purity: 99.03%
- CAS No.: 2595365-41-4
- 화학식: C36H36N10O5
- 분자량:688.74
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biological Activity
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JAK2 |
SJ988497 (compound 7) increases cell permeability in the Caco-2 assay, with the apparent permeability coefficient (Papp) of 19.12 nm/s[1].
SJ988497 inhibits parental MHH-CALL-4 cells with an EC50 of 0.4 nM, inhibits CRBN-KD MHH–CALL-4 cells with an EC50 of 3456.2 nM, and can be blocked by 30 μM Lenalidomide (HY-A0003)[1].
SJ988497 (1 h, 1 μM) results in comparable JAK inhibition in MHH–CALL-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NAL M6, MHH-CALL-2, 697, KOPN49, KOPN75, MHH-CALL-4 cells
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Concentration:0.01 nM-100 nM
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Incubation Time:72 h
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Result:Dose-dependently inhibited cell viability in ALL cell lines.
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Cell Line:MHH-CALL-4 cells
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Concentration:1 nM, 10 nM, 100 nM, 1 μM, 4 μM.
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Incubation Time:1 h
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Result:Degraded multiple JAKs (JAK1>JAK3>JAK2>TYK2), and was abolished by knockdown of CRBN.
SJ988497 (10-100 mg/kg, i.p., twice daily) showed sustained in vivo exposure with the plasma concentration above the cellular 50% effective concentration value after 24 hour[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice inoculated by CL20SF2-Luc2aYFP cell (i.v.)[1]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced leukemia burden in bone marrow, blood, and spleen, as well as total body bioluminescent imaging.
Chemical Information
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CAS No. 2595365-41-4
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Appearance Solid
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분자량 688.74
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화학식 C36H36N10O5
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Color Light yellow to yellow
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SMILES
CCCN1C=C(C=N1)C2=C3C=CNC3=NC(NC4=CC=C(C=C4)C(NCCCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=N2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 33.33 mg/mL (48.39 mM; ultrasonic and warming and heat to 80°C; 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.63 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 |
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| DMSO | 1 mM | 1.4519 mL | 7.2596 mL | 14.5193 mL | 36.2982 mL |
| 5 mM | 0.2904 mL | 1.4519 mL | 2.9039 mL | 7.2596 mL | |
| 10 mM | 0.1452 mL | 0.7260 mL | 1.4519 mL | 3.6298 mL | |
| 15 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4199 mL | |
| 20 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL | 1.8149 mL | |
| 25 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4519 mL | |
| 30 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2099 mL | |
| 40 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9075 mL |
SJ988497 Related Classifications
HY-151902 Related Classifications
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