UNC2881

Alias: UNC-2881; UNC 2881; UNC2881
Cat No.:V0637 Purity: ≥98%
UNC2881 (UNC-2881) is a novel, potent and specific Mer tyrosine kinase inhibitor with potential utility for prevention and treatment of pathologic thrombosis.
UNC2881 Chemical Structure CAS No.: 1493764-08-1
Product category: TAM Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

UNC2881 (UNC-2881) is a novel, potent and specific Mer tyrosine kinase inhibitor with potential utility for prevention and treatment of pathologic thrombosis. It exhibits 83- and 58-fold higher selectivity over Tyro3 and Axl, respectively, and inhibits Mer with an IC50 of 4.3 nM. Since Mer kinase controls the second stage of platelet activation, using Mer inhibitors to prevent thrombosis with a lower risk of bleeding than existing treatments presents an opportunity.

Biological Activity I Assay Protocols (From Reference)
Targets
Mer (IC50 = 4.3 nM); Axl (IC50 = 360 nM); Tyro (IC50 = 250 nM)
ln Vitro
UNC2881 (compound 23) (0-1000 nM; 1 h) inhibits ligand-stimulated EGFR-MerTK chimeric activation. UNC2881 also prevents acute lymphoblastic leukemia cells from having their natural Mer tyrosine kinase activated[1].
UNC2881 (3 μM; 1 h) suppresses platelet aggregation by more than 25% in response to fibrillar type I equine collagen stimulation in human platelet-rich plasma[1].
ln Vivo
UNC2881 (3 mg/kg; p.o.; single dose) exhibits a terminal half-life of 0.80 hours and a high systemic clearance of 94.5 mL/min/kg in addition to a 14% oral bioavailability[1].
UNC2881 (3 mg/kg; i.v.; injected with VSV on days -3, -2, -1, and 0) suppresses Mertk signaling and enhances the antiviral immune response, thereby decreasing the amount of VSV that replicates in infected mice[2].
Enzyme Assay
UNC2881 is a potent and selective inhibitor of Mer kinase that, at an IC50 of 22 nM, prevents steady-state Mer kinase phosphorylation.
Cell Assay
UNC2881 inhibited Mer phosphorylation in 697 B-ALL cells with an IC50 value of 22 nM. Moreover, UNC2881 prevented the ligand-dependent phosphorylation of a chimeric protein made up of the extracellular domain of the EGFR and the intracellular domain of Mer. UNC2881 prevented platelet aggregation caused by fibrillar Type I equine collagen in human platelet-rich plasma by more than 25%. Additionally, UNC2881 suppressed the release of ATP, a sign of activated platelets.
Animal Protocol
C57BL/6 mice (7-10 weeks old)[2]
3 mg/kg
Intravenous injection; infected with 2×108 PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0
References

[1]. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700.

[2]. Dead Cells Induce Innate Anergy Via Mertk after Acute Viral Infection. Cell Reports. 2020. 30(11):3671-3681.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H33N7O2
Molecular Weight
463.58
Exact Mass
463.27
Elemental Analysis
C, 64.77; H, 7.18; N, 21.15; O, 6.90
CAS #
1493764-08-1
Appearance
White solid powder
SMILES
CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C(=O)NCC3=CC=C(C=C3)N4C=CN=C4
InChi Key
NPVXOWLPOFYACO-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H33N7O2/c1-2-3-12-27-25-29-16-22(23(31-25)30-19-6-10-21(33)11-7-19)24(34)28-15-18-4-8-20(9-5-18)32-14-13-26-17-32/h4-5,8-9,13-14,16-17,19,21,33H,2-3,6-7,10-12,15H2,1H3,(H,28,34)(H2,27,29,30,31)
Chemical Name
2-(butylamino)-4-[(4-hydroxycyclohexyl)amino]-N-[(4-imidazol-1-ylphenyl)methyl]pyrimidine-5-carboxamide
Synonyms
UNC-2881; UNC 2881; UNC2881
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~292 mg/mL (~198.5 mM)
Water: <1 mg/mL
Ethanol: ~5 mg/mL(~10.8 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1571 mL 10.7856 mL 21.5712 mL
5 mM 0.4314 mL 2.1571 mL 4.3142 mL
10 mM 0.2157 mL 1.0786 mL 2.1571 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • UNC2881

    UNC2881 (compound 23) inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells.J Med Chem.2013 Dec 12;56(23):9693-700.

  • UNC2881


    UNC2881

    23 inhibits ligand-stimulated activation of a chimeric EGFR-MerTK.J Med Chem.2013 Dec 12;56(23):9693-700.

  • UNC2881

    23 inhibits collagen-stimulated platelet aggregation.J Med Chem.2013 Dec 12;56(23):9693-700.

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