1400687-19-5

1400687-19-5 structure

Name: JAK-IN-35
Chemical Name: 4-{[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino}-6-(6-methoxy-3-pyridinyl)pyrrolo[1,2-b]pyridazine-3-carboxamide
CAS Number: 1400687-19-5
Molecular Formula: C₂₂H₂₈N₆O₂
Molecular Weight: 408.497
Create Date: 2020-01-11 17:35:51
Modify Date: 2024-01-04 11:32:28
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.

Name	4-{[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino}-6-(6-methoxy-3-pyridinyl)pyrrolo[1,2-b]pyridazine-3-carboxamide
Synonyms	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)-

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