A JAK1 inhibitor
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AZD 4604

Item No. 39890

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[5-fluoro-2-[[2-fluoro-3-(methylsulfonyl)phenyl]amino]-4-pyrimidinyl]-1H-indol-7-yl]-αR-(methoxymethyl)-4-methyl-1-piperazineacetamide
CAS Number
2241039-81-4
Synonyms
  • Londamocitinib
Molecular Formula
C28H31F2N7O4S
Formula Weight
599.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
FC1=C(C2=CNC3=C2C=CC=C3NC([C@@H](COC)N4CCN(C)CC4)=O)N=C(NC5=C(F)C(S(C)(=O)=O)=CC=C5)N=C1
InChi Code
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
InChi Key
JNUZADQZHYFJGW-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $109

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    5 mg

    $436

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    10 mg

    $654

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    50 mg

    $1,089

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    Product Description

    AZD 4604 is a JAK1 inhibitor (IC50 = 0.54 nM).1 It is selective for JAK1 over JAK2 and JAK3 (IC50s = 686 and >10,000 nM, respectively), as well as tyrosine kinase 2 (TYK2; IC50 = 657 nM). AZD 4604 inhibits IL-4- or IL-13-induced phosphorylation of STAT6 in U937 cells (IC50s = 24 and 34 nM, respectively). In vivo, AZD 4604 (1 mg/kg) reduces lung STAT3 and STAT5 phosphorylation in a rat model of ovalbumin-induced asthma.2 It also inhibits lung eosinophilia and reduces the late asthmatic response in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nilsson, M., Berggren, K., Berglund, S., et al. Discovery of the potent and selective inhaled janus kinase 1 inhibitor AZD4604 and its preclinical characterization. J. Med. Chem. 66(19), 13400-13415 (2023).

    2. Nilsson, M., Rhedin, M., Hendrickx, R., et al. Characterization of selective and potent JAK1 inhibitors intended for the inhaled treatment of asthma. Drug Des. Devel. Ther. 16, 2901-2917 (2022).