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| 25mg |
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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. 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.
| Targets |
Mer (IC50 = 4.3 nM); Axl (IC50 = 360 nM); Tyro (IC50 = 250 nM)
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| 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.
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| 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.
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| 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 |
| Molecular Formula |
C25H33N7O2
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|---|---|---|
| Molecular Weight |
463.58
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| Exact Mass |
463.269
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| Elemental Analysis |
C, 64.77; H, 7.18; N, 21.15; O, 6.90
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| CAS # |
1493764-08-1
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| Related CAS # |
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| PubChem CID |
71721525
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| Appearance |
White solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.666
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| LogP |
3.03
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
608
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N([H])C1C(C(N([H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])N2C([H])=NC([H])=C2[H])=O)=C([H])N=C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N=1
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| InChi Key |
NPVXOWLPOFYACO-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
2-(butylamino)-4-[(4-hydroxycyclohexyl)amino]-N-[(4-imidazol-1-ylphenyl)methyl]pyrimidine-5-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
UNC2881 (compound 23) inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells.J Med Chem.2013 Dec 12;56(23):9693-700. |
23 inhibits ligand-stimulated activation of a chimeric EGFR-MerTK.J Med Chem.2013 Dec 12;56(23):9693-700. |
23 inhibits collagen-stimulated platelet aggregation.J Med Chem.2013 Dec 12;56(23):9693-700. |
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