GLPBio

UNC569

Catalog No.: GC18308Purity:>98.50%
COASDSData Sheet
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.

UNC569
Cas No.: 1350547-65-7
10mM (in 1mL DMSO)In Stock
$85.00
1
1mgIn Stock
$35.00
1
5mgIn Stock
$77.00
1
10mgIn Stock
$126.00
1
25mgIn Stock
$280.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

No citations are currently available for this product. Below are selected publications citing GlpBio products.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Description

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.

Protocol

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:
[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] 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.

Product Documents

Purity:>98.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1350547-65-7
Chemical Name
1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
SMILES
CCCCNC1=NC=C2C(N(C[C@H]3CC[C@H](N)CC3)N=C2C4=CC=C(F)C=C4)=N1
Molecular Formula
C22H29FN6
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

Reviews

Review for UNC569

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%