UNC569
Based on 2 publication(s) in Google Scholar
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
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- Pureza: 99.92%
- No. CAS: 1350547-65-7
- Fòrmula: C22H29FN6
- Peso molecular:396.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) UNC569
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Actividad biológica
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Axl |
Tyro3 |
Mer |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
141 nM
Compound: 43, UNC569
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Inhibition of Mer autophosphorylation in human 697 cells pretreated for 1 hr before addition of phosphatase inhibitor measured by Western blot analysis
Inhibition of Mer autophosphorylation in human 697 cells pretreated for 1 hr before addition of phosphatase inhibitor measured by Western blot analysis
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[PMID: 22662287] |
UNC569 (24 hours) induces apoptosis in ALL cell lines, and increases the levels of cleaved Caspase 3 and cleaved PARP[2].
UNC569 (1 μM; 1.5 hours) treatment effectively inhibit the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways[2].
UNC569 (1 hour) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, respectively[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:697 and Jurkat cells
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Concentration:0.4 µM, 0.8 µM, 1 µM, 1.2 µM, 1.4 µM, 1.6 µM, 1.8 µM, 2 µM
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Incubation Time:24 hours
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Result:Induced apoptosis in ALL cell lines.
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Cell Line:697 and Jurkat cells
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Concentration:1 µM
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Incubation Time:1.5 hours
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Result:Inhibited Mer activation and downstream signaling through ERK1/2 and AKT.
Leukemic zebrafish are treated continuously for 2 weeks by immersion in 4 μM UNC569. the result shows that UNC569 induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1350547-65-7
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Appearance Solid
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Peso molecular 396.50
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Fòrmula C22H29FN6
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Color White to yellow
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SMILES
FC1=CC=C(C2=NN(C[C@H]3CC[C@H](N)CC3)C4=NC(NCCCC)=NC=C42)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
Tomentosin suppressed M1 polarization via increasing MERTK activation mediated by regulation of GAS6. [Abstract]2023 Oct 5:314:116429. PMID: 37011736 -
Bioorg Med Chem
Identification of a novel Aurora B inhibitor using the AI-driven drug screening and docking-based traditional screening. [Abstract]2025 Sep 27:131:118423. PMID: 41033076
Solvente y solubilidad
DMSO : 31.25 mg/mL (78.81 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. 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 (6.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jing Liu, et al. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett. 2012 Feb 9;3(2):129-134. [Content Brief]
[2]. Sandra Christoph, et al. UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77. [Content Brief]
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 | 2.5221 mL | 12.6103 mL | 25.2207 mL | 63.0517 mL |
| 5 mM | 0.5044 mL | 2.5221 mL | 5.0441 mL | 12.6103 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5221 mL | 6.3052 mL | |
| 15 mM | 0.1681 mL | 0.8407 mL | 1.6814 mL | 4.2034 mL | |
| 20 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL | 3.1526 mL | |
| 25 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5221 mL | |
| 30 mM | 0.0841 mL | 0.4203 mL | 0.8407 mL | 2.1017 mL | |
| 40 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5763 mL | |
| 50 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 60 mM | 0.0420 mL | 0.2102 mL | 0.4203 mL | 1.0509 mL |
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