CAS 1493694-70-4|UNC2250

Introduction：Basic information about CAS 1493694-70-4|UNC2250, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. UNC2250 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	UNC2250
CAS Number	1493694-70-4	Molecular Weight	440.582
Density	1.2±0.1 g/cm3	Boiling Point	657.4±65.0 °C at 760 mmHg
Molecular Formula	C₂₄H₃₆N₆O₂	Melting Point	/
MSDS	/	Flash Point	351.4±34.3 °C

Names

Name	4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol
Synonym	More Synonyms

UNC2250 BiologicalActivity

Description	UNC2250 is a phosphorylation of endogenous Mer inhibitor with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein.IC50 Value: 9.8 nM [1]Target: Othersin vitro: UNC2250 is 160-fold more active for Mer versus Axl and 60-fold versus Tyro3. UNC2250 had a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility and was thus chosen for characterization of kinase selectivity and further evaluation in cell-based studies of Mer activity. UNC2250 efficiently inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer. Moreover, UNC2250 incubation inhibited colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines. In the Colo699 NSCLC cell line, the concentrations of UNC2250 required to inhibit colony formation and Mer phosphorylation were similar. These data suggest that the functional antiproliferative activity mediated by UNC2250 resulted from Mer inhibition rather than a consequence of off-target inhibition of other kinases [1,2].In vivo:
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>TAM ReceptorResearch Areas >>Cancer
References	[1]. Zhang, W., et al., Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem, 2013. 56(23): p. 9683-92. [2]. http://www.google.com/patents/WO2013177168A1

Description

UNC2250 is a phosphorylation of endogenous Mer inhibitor with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein.IC50 Value: 9.8 nM [1]Target: Othersin vitro: UNC2250 is 160-fold more active for Mer versus Axl and 60-fold versus Tyro3. UNC2250 had a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility and was thus chosen for characterization of kinase selectivity and further evaluation in cell-based studies of Mer activity. UNC2250 efficiently inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer. Moreover, UNC2250 incubation inhibited colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines. In the Colo699 NSCLC cell line, the concentrations of UNC2250 required to inhibit colony formation and Mer phosphorylation were similar. These data suggest that the functional antiproliferative activity mediated by UNC2250 resulted from Mer inhibition rather than a consequence of off-target inhibition of other kinases [1,2].In vivo:

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>TAM ReceptorResearch Areas >>Cancer

References

[1]. Zhang, W., et al., Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem, 2013. 56(23): p. 9683-92.

[2]. http://www.google.com/patents/WO2013177168A1

Chemical & Physical Properties

Density	1.2±0.1 g/cm3
Boiling Point	657.4±65.0 °C at 760 mmHg
Molecular Formula	C₂₄H₃₆N₆O₂
Molecular Weight	440.582
Flash Point	351.4±34.3 °C
Exact Mass	440.289978
PSA	101.89000
LogP	0.79
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.626
InChIKey	HSYSSKFCQHXOBP-UHFFFAOYSA-N
SMILES	CCCCNc1ncc(-c2ccc(CN3CCOCC3)cn2)c(NC2CCC(O)CC2)n1
Storage condition	2-8°C

Synonyms

Cyclohexanol, 4-[[2-(butylamino)-5-[5-(4-morpholinylmethyl)-2-pyridinyl]-4-pyrimidinyl]amino]-, trans-

trans-4-({2-(Butylamino)-5-[5-(4-morpholinylmethyl)-2-pyridinyl]-4-pyrimidinyl}amino)cyclohexanol

UNC2250

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