UNC569 |
Catalog No.GC18308
One-Click Copy Product Info
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UNC569 is a novel small molecule Mer tyrosine kinase inhibitor with potent activity against Mer (Mer IC50 = 2.9nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1350547-65-7
Sample solution is provided at 25 µL, 10mM.
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UNC569 is a novel small molecule Mer tyrosine kinase inhibitor with potent activity against Mer (Mer IC50 = 2.9nM)[1].
In vitro, UNC569 (0, 400, 800, 1000, 1200, 1400, 1600, 1800, and 2000nM; 48h) reduces proliferation and induces apoptosis in acute lymphoblastic leukemia (ALL) cells[1]. In macrophages derived from THP-1 cells, UNC569 (5μM; 48h) significantly inhibits Gas-6-induced MerTK phosphorylation and Akt activation[2]. In the presence and absence of exogenous galectin-3, UNC569 (5μM; 48h) strongly inhibited microglial phagocytosis of bacteria, without affecting microglial viability[3].
In vivo, In a mouse animal experiment, the MerTK inhibitor UNC569 (60, 100 and 150mg/kg or 100mg/kg; 14 days or 15, 17, 18.5 and 20h; p.o.) impaired the phagocytic function of the retinal pigment epithelium (RPE), leading to accumulation of photoreceptor outer segments (POS) and increased phagosomes and phagolysosomes in the RPE[4].
References:
[1] Christoph S, Deryckere D, 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.
[2] Pastore M, Caligiuri A, Raggi C, et al. Macrophage MerTK promotes profibrogenic cross-talk with hepatic stellate cells via soluble mediators. JHEP Rep. 2022 Feb 1;4(4):100444.
[3] Cockram TOJ, Puigdellívol M, Brown GC. Calreticulin and Galectin-3 Opsonise Bacteria for Phagocytosis by Microglia. Front Immunol. 2019 Nov 12;10:2647.
[4] Sayama A, Okado K, Nakamura K, et al. UNC569-induced Morphological Changes in Pigment Epithelia and Photoreceptor Cells in the Retina through MerTK Inhibition in Mice. Toxicol Pathol. 2018 Feb;46(2):193-201.
| Cell experiment [1]: | |
Cell lines | Jurkat or 697 cells |
Preparation Method | Jurkat or 697 cells were plated at a density of 3×10⁵ cells/ml and treated with UNC569 (0, 400, 800, 1000, 1200, 1400, 1600, 1800 and 2000nM) for 48h. Alternatively, cells were treated with UNC569 for 24h, then harvested and cultured in fresh medium containing UNC569 or vehicle only for an additional 24h. Cells were collected by centrifugation at 240g for 5min. Cell pellets were resuspended in PBS containing 1µM YO-PRO-1 and 1.5µM propidium iodide. Samples were incubated for 15min, and fluorescence was detected using a FC500 flow cytometer and analyzed with CXP data analysis software. |
Reaction Conditions | 0, 400, 800, 1000, 1200, 1400, 1600, 1800 and 2000nM; 48h |
Applications | UNC569 reduces proliferation and induces apoptosis in acute lymphoblastic leukemia (ALL) cells. |
| Animal experiment [2]: | |
Animal models | Male BALB/c AnNCrlCrlj mice |
Preparation Method | UNC569 was administered orally once daily at doses of 60, 100, and 150mg/kg for 14 days. Animals receiving 0.5 w/v% methyl cellulose in the same manner served as the control group. During the experiment, light was introduced into the room at 7:00, and dosing was conducted at 10:30. The first day of dosing was defined as day 1. Animals were euthanized by exsanguinations under isoflurane anesthesia and necropsied at 10:30 on day 15. Eyes were removed from all animals. The right eyes were fixed in Davidson’s fixative, embedded in paraffin, and prepared as histopathological specimens, which were stained with hematoxylin and eosin (HE) for light microscopy. The left eyes were fixed in 2.5% glutaraldehyde, postfixed in 2% osmium tetroxide, and embedded in resin. Semithin sections were stained with toluidine blue (TB) for light microscopy, and ultrathin sections were stained with uranyl acetate and lead for electron microscopy. |
Dosage form | 60, 100 and 150mg/kg; 14 days; p.o. |
Applications | In a mouse animal experiment, the MerTK inhibitor UNC569 impaired the phagocytic function of the retinal pigment epithelium (RPE), leading to accumulation of photoreceptor outer segments (POS) and increased phagosomes and phagolysosomes in the RPE. |
References: | |
| Cas No. | 1350547-65-7 | SDF | |
| Chemical Name | 1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine | ||
| Canonical SMILES | CCCCNC1=NC=C2C(N(C[C@H]3CC[C@H](N)CC3)N=C2C4=CC=C(F)C=C4)=N1 | ||
| Formula | C22H29FN6 | M.Wt | 396.5 |
| Solubility | DMF: 2.5 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml,DMSO: 0.2 mg/ml,Ethanol: 2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5221 mL | 12.6103 mL | 25.2207 mL |
| 5 mM | 504.4 μL | 2.5221 mL | 5.0441 mL |
| 10 mM | 252.2 μL | 1.261 mL | 2.5221 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)