Purinostat mesylate
Based on 1 Customer Validation
Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 2650188-32-0
- Formula: C24H30N10O6S
- Molecular Weight:586.62
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
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HDAC1 0.81 nM (IC50) |
HDAC10 1.1 nM (IC50) |
HDAC2 1.4 nM (IC50) |
HDAC3 1.7 nM (IC50) |
HDAC8 3.8 nM (IC50) |
HDAC6 11.5 nM (IC50) |
HDAC5 426 nM (IC50) |
HDAC7 590 nM (IC50) |
HDAC9 622 nM (IC50) |
HDAC4 1072 nM (IC50) |
HDAC11 3349 nM (IC50) |
Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3 and 8 with IC50s of 0.81, 1.4, 1.7 and 3.8 nM, inhibits HDAC6 and 10 with IC50s of 11.5 and 1.1 nM, and inhibits HDAC4, 5, 7, 9 and 11 with IC50s of 1072, 426, 690, 622 and 3348 nM, respectively[1]. Purinostat mesylate (0-60 nM; 24 h) induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LAMA84 and 188 BL-2 cell lines
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Concentration:0-80 nM
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Incubation Time:24, 48 and 72 hours
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Result:Significantly inhibited cell proliferation of LAMA84 and 188 BL-2 cells.
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Cell Line:LAMA84 and 188 BL-2 cell lines
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Concentration:0-60 nM
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Incubation Time:24 hours
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Result:Induced apoptosis of LAMA84 and 188 BL-2 cells.
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Cell Line:LAMA84 and 188 BL-2 cell lines
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Concentration:0-40 nM
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Incubation Time:24 hours
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Result:Dose-dependently blocked cell cycle progression at G0/G1 phase.
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Cell Line:LAMA84 and 188 BL-2 cell lines
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Concentration:0-40 nM
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Incubation Time:24 hours
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Result:Dose-dependently increased the 191 levels of Ac-H3 and Ac-H4, and decreased HSP90.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Non-irradiated C57BL/6 recipient mice with BL-2 cells injection[1]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneal injection; 5-10 mg/kg three times a week; for five weeks
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Result:Significantly prolonged the overall survival rate and suppressed leukemia progression of mice, and no tumor cell was detected after stopped treatment.
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Animal Model:Non-irradiated C57BL/6 recipient mice with BL-2 secondary transplantation[1]
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Dosage:10 mg/kg
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Administration:Intravenous injection; 10 mg/kg three times a week
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Result:Completely eliminated GFP+B220+ cells in spleens on day 3 with two times treatment and this complete inhibition was maintained for 26 days duration of treatment.
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Animal Model:B-ALL mouse with BCR-ABL(T315I)-induced leukemia[1]
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Dosage:5 and 10 mg/kg
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Administration:Intravenous injection; 5 and 10 mg/kg three times a week; for 8 weeks
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Result:Significantly prolonged survival rate of BCR-ABL(T315I)-induced B-ALL mice. Survived all mice after treatment for 42 days.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2650188-32-0
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Appearance Solid
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Molecular Weight 586.62
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Formula C24H30N10O6S
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Color Off-white to light yellow
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SMILES
O=C(C1=CN=C(N(CC2=NC3=C(N4CCOCC4)N=C(C5=CC=C(N)C=C5)N=C3N2C)C)N=C1)NO.O=S(O)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 35 mg/mL (59.66 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.
Add each solvent one by one: 5% PEG300 95% Saline
Solubility: 3.33 mg/mL (5.68 mM); Suspended solution; Need ultrasonic
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.7047 mL | 8.5234 mL | 17.0468 mL | 42.6170 mL |
| 5 mM | 0.3409 mL | 1.7047 mL | 3.4094 mL | 8.5234 mL | |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7047 mL | 4.2617 mL | |
| 15 mM | 0.1136 mL | 0.5682 mL | 1.1365 mL | 2.8411 mL | |
| 20 mM | 0.0852 mL | 0.4262 mL | 0.8523 mL | 2.1309 mL | |
| 25 mM | 0.0682 mL | 0.3409 mL | 0.6819 mL | 1.7047 mL | |
| 30 mM | 0.0568 mL | 0.2841 mL | 0.5682 mL | 1.4206 mL | |
| 40 mM | 0.0426 mL | 0.2131 mL | 0.4262 mL | 1.0654 mL | |
| 50 mM | 0.0341 mL | 0.1705 mL | 0.3409 mL | 0.8523 mL |