UNC9750
Based on 1 Customer Validation
UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC50 values of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP5, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP7 levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma.
For research use only. We do not sell to patients.
- Purity : 96.50%
- CAS No.: 2967648-29-7
- Formula: C23H24N6O
- Molecular Weight:400.48
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
[1]|
DYRK1B |
DAPK1 |
PDGFR |
PDGFR2 |
In Vitro
UNC9750 (Compound 14) (0-10 μM, 48-72 h) decreases human glioblastoma cell U251-MG growth and selectively reduces cellular InsP5 abundance but does not decrease InsP6 or InsP7 levels after 72 h[1].
UNC9750 (1 μM) has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR[1].
UNC9750 (10-50 μM, 24 h) can significantly and concentration-dependently upregulate the expression of SF-1 target gene CYP11A1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUClast | Vss | CL |
|---|---|---|---|---|---|---|---|
| Mice[1] | 2.75 mg/kg | i.v. | 1.95 h | 28.3 μM | 4.6 μM·h | 0.39 L/kg | 22.8 mL/min/kg |
Chemical Information
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CAS No. 2967648-29-7
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Appearance Solid
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Molecular Weight 400.48
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Formula C23H24N6O
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SMILES
C1(C2=NN=NN2)=CC3=C(ON=C3C=C1)C4=CC(C5CCN(CC5)C6CCC6)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 8.33 mg/mL (20.80 mM; Need warming; 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)
In Vivo:
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: ≥ 0.83 mg/mL (2.07 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.07 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
In Vivo Dissolution Calculator
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
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 | 2.4970 mL | 12.4850 mL | 24.9700 mL | 62.4251 mL |
| 5 mM | 0.4994 mL | 2.4970 mL | 4.9940 mL | 12.4850 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4970 mL | 6.2425 mL | |
| 15 mM | 0.1665 mL | 0.8323 mL | 1.6647 mL | 4.1617 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2485 mL | 3.1213 mL |
Keywords
- UNC9750
- 2967648-29-7
- UNC 9750
- UNC-9750
- DAPK
- DYRK
- PDGFR
- IPK Superfamily
- Death associated protein kinase
- Dual specificity tyrosine phosphorylation regulated kinase
- Dual specificity tyrosine regulated kinase
- Platelet-derived growth factor receptor
- Inositiol Polyphosphate Kinase (IPK) Superfamily
- U251-MG glioblastoma cells
- Inositol phosphate metabolism
- Inhibitor
- inhibitor
- inhibit