For research use only. Not for therapeutic Use.
Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity[1][2][3].
Londamocitinib inhibits the phosphorylation of STAT6 in U937 cells induced by IL-4 or IL-13 (IC50 are 24 and 34 nM, respectively)[2].
Londamocitinib (1 mg/kg, intravenous injection, single dose) can reduce the phosphorylation of STAT3 and STAT5 in the lung of obumin-induced asthmatic rats, inhibit pulmonary eosinophilia, and reduce advanced asthma response in the same model[3].
| Catalog Number | I018683 |
| CAS Number | 2241039-81-4 |
| Synonyms | (2R)-N-[3-[5-fluoro-2-(2-fluoro-3-methylsulfonylanilino)pyrimidin-4-yl]-1H-indol-7-yl]-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide |
| Molecular Formula | C28H31F2N7O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C28H31F2N7O4S/c1-36-10-12-37(13-11-36)22(16-41-2)27(38)33-21-8-4-6-17-18(14-31-26(17)21)25-19(29)15-32-28(35-25)34-20-7-5-9-23(24(20)30)42(3,39)40/h4-9,14-15,22,31H,10-13,16H2,1-3H3,(H,33,38)(H,32,34,35)/t22-/m1/s1 |
| InChIKey | JNUZADQZHYFJGW-JOCHJYFZSA-N |
| SMILES | CN1CCN(CC1)C(COC)C(=O)NC2=CC=CC3=C2NC=C3C4=NC(=NC=C4F)NC5=C(C(=CC=C5)S(=O)(=O)C)F |
| Reference | [1]. NILSSON, Karl, Magnus, et al. Jak1 selective inhibitors. WO2018134213A1. [2]. Nilsson M, et al. Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization. J Med Chem. 2023 Oct 12;66(19):13400-13415. [3]. Nilsson M, et al. Characterization of Selective and Potent JAK1 Inhibitors Intended for the Inhaled Treatment of Asthma. Drug Des Devel Ther. 2022 Aug 31;16:2901-2917. |
