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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
UNC2250 UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
Targets
Axl ; Axl ; Mer ; Tyro3 ; 1.7 nM; 100 nM
In vitro
UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells.
In vivo
According to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility.
Cell Research(from reference)
Cell lines：BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells
Concentrations：~3 μM for BT-12, ~300 nM for Colo699
Incubation Time：3 weeks for BT-12, 2 weeks for Colo699
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Spezifikationsblatt ansehen →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Klasse | Diazines |
| Subclass | Pyrimidines and pyrimidine derivatives |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Aminopyrimidines and derivatives |
| Alternative Parents | Secondary alkylarylamines Cyclohexanols Aralkylamines Pyridines and derivatives Morpholines Imidolactams Heteroaromatic compounds Trialkylamines Cyclic alcohols and derivatives Oxacyclic compounds Dialkyl ethers Azacyclic compounds Organopnictogen compounds Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Aralkylamine - Secondary aliphatic/aromatic amine - Cyclohexanol - Aminopyrimidine - Imidolactam - Pyridine - Oxazinane - Morpholine - Heteroaromatic compound - Cyclic alcohol - Tertiary aliphatic amine - Tertiary amine - Secondary alcohol - Oxacycle - Azacycle - Secondary amine - Ether - Dialkyl ether - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Amine - Alcohol - Aromatic heteromonocyclic compound |
| Beschreibung | This compound belongs to the class of organic compounds known as aminopyrimidines and derivatives. These are organic compounds containing an amino group attached to a pyrimidine ring. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions. |
| External Descriptors | Not available |
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| Molekulargewicht | 440.600 g/mol |
|---|---|
| XLogP3 | 2.800 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 9 |
| Exact Mass | 440.29 Da |
| Monoisotopic Mass | 440.29 Da |
| Topological Polar Surface Area | 95.400 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 527.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
