UNC2250Mer inhibitor,potent and selective CAS# 1493694-70-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1493694-70-4 | SDF | Download SDF |
| PubChem ID | 73211763 | Appearance | Powder |
| Formula | C24H36N6O2 | M.Wt | 440.58 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 20 mg/mL (45.39 mM; ultrasonic and warming and heat to 60°C) 0.1 M HCL : 12.5 mg/mL (28.37 mM; ultrasonic and adjust pH to 3 with HCl) | ||
| Chemical Name | 4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol | ||
| SMILES | CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4 | ||
| Standard InChIKey | HSYSSKFCQHXOBP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29) | ||
| 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 | UNC2250 is a potent and selective inhibitor of Mer with an IC50 value of 1.7 nM. | |||||
| Targets | Mer | |||||
| IC50 | 1.7 nM | |||||
UNC2250 Dilution Calculator
UNC2250 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2697 mL | 11.3487 mL | 22.6974 mL | 45.3947 mL | 56.7434 mL |
| 5 mM | 0.4539 mL | 2.2697 mL | 4.5395 mL | 9.0789 mL | 11.3487 mL |
| 10 mM | 0.227 mL | 1.1349 mL | 2.2697 mL | 4.5395 mL | 5.6743 mL |
| 50 mM | 0.0454 mL | 0.227 mL | 0.4539 mL | 0.9079 mL | 1.1349 mL |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.227 mL | 0.4539 mL | 0.5674 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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UNC2250 is a highly selective inhibitor of Mer receptor tyrosine kinase with IC50 value of 1.7nM [1].
UNC2250 shows a potent inhibitory activity against Mer with IC50 value of 1.7nM. The IC50 values for other TAM kinases such as Axl and Tyro3 are 270nM and 100nM, respectively. In addition, UNC2250 shows no significant inhibition of a panel of 30 other kinases. In cell-based assays, UNC2250 inhibits the phosphorylation of Mer with IC50 value of 9.8nM in B-ALL cells. It also prevents the colony formation both in BT-12 cell lines and in Colo699 NSCLC cell lines. Furthermore, UNC2250 is proved to have a moderate half-life, clearance, distribution volume and good oral bioavailability [1].
References:
[1] Zhang W, Zhang D, Stashko M A, et al. Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors. Journal of medicinal chemistry, 2013, 56(23): 9683-9692.
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Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.[Pubmed:24195762]
J Med Chem. 2013 Dec 12;56(23):9683-92.
Abnormal activation or overexpression of Mer receptor tyrosine kinase has been implicated in survival signaling and chemoresistance in many human cancers. Consequently, Mer is a promising novel cancer therapeutic target. A structure-based drug design approach using a pseudo-ring replacement strategy was developed and validated to discover a new family of pyridinepyrimidine analogues as potent Mer inhibitors. Through SAR studies, 10 (UNC2250) was identified as the lead compound for further investigation based on high selectivity against other kinases and good pharmacokinetic properties. When applied to live cells, 10 inhibited steady-state phosphorylation of endogenous Mer with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein. Treatment with 10 also resulted in decreased colony-forming potential in rhabdoid and NSCLC tumor cells, thereby demonstrating functional antitumor activity. The results provide a rationale for further investigation of this compound for therapeutic application in patients with cancer.
