mrx-6313

Names

[ Name ]:
mrx-6313

[Synonym ]:
UNC2025
Cyclohexanol, 4-[2-(butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans-
trans-4-[2-(Butylamino)-5-{4-[(4-methyl-1-piperazinyl)methyl]phenyl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol
UNC-2025
UNC2025 hydrochloride

Biological Activity

[Description]:

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.IC50 value: 0.8/0.74 nM(MER/FLT3)Target: Mer/Flt3 inhibitorUNC2025 was capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome pro ling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that 11 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

Research Areas >> Cancer

[References]

[1]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
677.5±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₈H₄₀N₆O

[ Molecular Weight ]:
476.657

[ Flash Point ]:
363.5±34.3 °C

[ Exact Mass ]:
476.326355

[ LogP ]:
3.09

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.655

[ Storage condition ]:
-20℃

Related Compounds

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