Sovleplenib
Based on 1 Customer Validation
Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 1415792-84-5
- Formula: C24H30N6O3S
- Molecular Weight:482.60
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
SYK[1]
Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC50s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively[1].
Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC50s of 0.105 μM and 0.173 μM, respectively[2].
Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC50 of 0.033 μM[2].
Sovleplenib also increases the apoptotic rate of REC-1 cells[2].
Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells[1]
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Dosage:10 and 100 mg/kg
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Administration:q.d.; for 8 days
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Result:Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1415792-84-5
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Appearance Solid
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Molecular Weight 482.60
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Formula C24H30N6O3S
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Color Light yellow to yellow
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SMILES
CS(N(CC1)CCC1C(C=C2)=CC=C2C3=CC(N=CC=N4)=C4C(NC[C@@H]5CNCCO5)=N3)(=O)=O
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Synonyms
HMPL-523
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (51.80 mM; ultrasonic and warming and heat to 60°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: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0721 mL | 10.3605 mL | 20.7211 mL | 51.8027 mL |
| 5 mM | 0.4144 mL | 2.0721 mL | 4.1442 mL | 10.3605 mL | |
| 10 mM | 0.2072 mL | 1.0361 mL | 2.0721 mL | 5.1803 mL | |
| 15 mM | 0.1381 mL | 0.6907 mL | 1.3814 mL | 3.4535 mL | |
| 20 mM | 0.1036 mL | 0.5180 mL | 1.0361 mL | 2.5901 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0721 mL | |
| 30 mM | 0.0691 mL | 0.3454 mL | 0.6907 mL | 1.7268 mL | |
| 40 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2951 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0361 mL |
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