JAK-IN-35
Names
[ CAS No. ]:
1400687-19-5
[ Name ]:
JAK-IN-35
[Synonym ]:
4-{[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino}-6-(6-methoxy-3-pyridinyl)pyrrolo[1,2-b]pyridazine-3-carboxamide
Pyrrolo[1,2-b]pyridazine-3-carboxamide, 4-[[(1R,3S)-3-amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-methoxy-3-pyridinyl)-
Biological Activity
[Description]:
JAK-IN-35 is a potent and efficacious dual JAK1/JAK3 inhibitor with IC50 of 0.9/1.9 nM; shows weak activity against TYK2 and JAK2 (IC50=25 nM and15 nM respectively), also inhibits both ROCK1 (IC50=95 nM) and ROCK2 (IC50=43 nM); inhibits JAK1/3 mediated ex vivo processes in the mouse PD model (EC50 67 ± 13 nM); shows potential cardiovascular liabilities, specifically, QT interval prolongation.
[References]
References 1. Hynes J Jr, et al. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. View Related Products by Target JAK
Chemical & Physical Properties
[ Density]:
1.4±0.1 g/cm3
[ Molecular Formula ]:
C22H28N6O2
[ Molecular Weight ]:
408.497
[ Exact Mass ]:
408.227386
[ LogP ]:
2.63
[ Index of Refraction ]:
1.673