UNC4203

Names

[ Name ]:
UNC4203

[Synonym ]:
trans-4-(5-{4-[(4-Methyl-1,4-diazepan-1-yl)methyl]phenyl}-2-[(2S)-2-pentanylamino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol
Cyclohexanol, 4-[5-[4-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)methyl]phenyl]-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans-

Biological Activity

[Description]:

UNC4203 (UNC-4203) is a potent, highly selective MerTK with IC50 of 2.4 nM, displays >30- and 4 -foldfold selectivity over Alx (IC50=80 nM) and Tyro3 (IC50=9.1 nM); display IC50 of 39 nM for FLT-3, inhibits MERTK phosphorylation in cell-based assays with IC50 of 13.8 nM, inhibits MERTK phosphorylation in vivo in mice with advanced leukemia (30 mg/kg, ip injection).

[References]

References 1. Zhao J, et al. J Med Chem. 2018 Nov 5. doi: 10.1021/acs.jmedchem.8b01229. View Related Products by Target TAM Receptor (Tyro3-Axl-Mer)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
682.0±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₀H₄₄N₆O

[ Molecular Weight ]:
504.710

[ Flash Point ]:
366.3±34.3 °C

[ Exact Mass ]:
504.357666

[ LogP ]:
4.18

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

[ Index of Refraction ]:
1.642

Related Compounds

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