UNC2881Mer tyrosine kinase inhibitor CAS# 1493764-08-1 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1493764-08-1 | SDF | Download SDF |
| PubChem ID | 71721525 | Appearance | Powder |
| Formula | C25H33N7O2 | M.Wt | 463.58 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 44 mg/mL (94.91 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-(butylamino)-4-[(4-hydroxycyclohexyl)amino]-N-[(4-imidazol-1-ylphenyl)methyl]pyrimidine-5-carboxamide | ||
| SMILES | CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C(=O)NCC3=CC=C(C=C3)N4C=CN=C4 | ||
| Standard InChIKey | NPVXOWLPOFYACO-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | UNC2881 is a specific inhibitor of Mer tyrosine kinase with IC50 value of 4.3 nM. | |||||
| Targets | Mer tyrosine kinase | |||||
| IC50 | 4.3 nM | |||||
UNC2881 Dilution Calculator
UNC2881 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1571 mL | 10.7856 mL | 21.5712 mL | 43.1425 mL | 53.9281 mL |
| 5 mM | 0.4314 mL | 2.1571 mL | 4.3142 mL | 8.6285 mL | 10.7856 mL |
| 10 mM | 0.2157 mL | 1.0786 mL | 2.1571 mL | 4.3142 mL | 5.3928 mL |
| 50 mM | 0.0431 mL | 0.2157 mL | 0.4314 mL | 0.8628 mL | 1.0786 mL |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2157 mL | 0.4314 mL | 0.5393 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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UNC2881 is a selective inhibitor of Mer tyrosine kinase [1].
Mer is a member of the TAM (Tyro3, Axl and Mer) receptor tyrosine kinase (RTK) subfamily with growth-arrest-specific-6 (Gas6) as an endogenous ligand. Mer plays an important role in platelet aggregation and macrophage activity.
UNC2881 is a novel and specific Mer tyrosine kinase inhibitor. In kinase inhibition assays, UNC2881 (430 nM) inhibited MER, FGFR1, KDR, EGFR, ITK and TRKA by greater than 50%. In 697 B-ALL cells, UNC2881 inhibited Mer phosphorylation with IC50 value of 22 nM. Also, UNC2881 inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the intracellular domain of Mer and the extracellular domain of the epidermal growth factor receptor (EGFR). In human platelet-rich plasma, UNC2881 inhibited platelet aggregation induced by fibrillar Type I equine collagen by greater than 25%. UNC2881 also inhibited ATP release, a marker of platelet activation [1].
In mice, UNC2881 exhibited 14% oral bioavailability and high systemic clearance. UNC2881 was sufficient for in vitro or short-term in vivo studies [1].
Reference:
[1]. Zhang W, McIver AL, Stashko MA, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem, 2013, 56(23): 9693-9700.
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Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.[Pubmed:24219778]
J Med Chem. 2013 Dec 12;56(23):9693-700.
The role of Mer kinase in regulating the second phase of platelet activation generates an opportunity to use Mer inhibitors for preventing thrombosis with diminished likelihood for bleeding as compared to current therapies. Toward this end, we have discovered a novel, Mer kinase specific substituted-pyrimidine scaffold using a structure-based drug design and a pseudo ring replacement strategy. The cocrystal structure of Mer with two compounds (7 and 22) possessing distinct activity have been determined. Subsequent SAR studies identified compound 23 (UNC2881) as a lead compound for in vivo evaluation. When applied to live cells, 23 inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. Treatment with 23 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, 23 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may have utility for prevention and/or treatment of pathologic thrombosis.
