A TYK2 inhibitor
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Zasocitinib

Item No. 35682

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1R,2R)-2-methoxycyclobutyl]-7-(methylamino)-5-[(2-oxo[1(2H),,wbr/>2′-bipyridin]-3-yl)amino]-pyrazolo[1,5-a]pyrimidine-3-carboxamide
CAS Number
2272904-53-5
Synonyms
  • NDI-034858
  • TAK-279
Molecular Formula
C23H24N8O3
Formula Weight
460.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
CO[C@H](CC1)[C@@H]1NC(C2=C3N(N=C2)C(NC)=CC(NC4=CC=CN(C5=CC=CC=N5)C4=O)=N3)=O
InChi Code
InChI=1S/C23H24N8O3/c1-24-20-12-18(27-16-6-5-11-30(23(16)33)19-7-3-4-10-25-19)29-21-14(13-26-31(20)21)22(32)28-15-8-9-17(15)34-2/h3-7,10-13,15,17,24H,8-9H2,1-2H3,(H,27,29)(H,28,32)/t15-,17-/m1/s1
InChi Key
BWINBHTTZLVXGT-NVXWUHKLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $299

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    Product Description

    Zasocitinib is an inhibitor of tyrosine kinase 2 (TYK2).1 It selectively binds to the TYK2 Janus homology (JH2) domain (Kd = 0.0038 nM) over the JAK1 and JAK2 JH2 domains (Kds = 4,975 and 23,000 nM, respectively). Zasocitinib inhibits the production of chemokine (C-X-C motif) ligand 10 (CXCL10) induced by IFN-α in isolated human, mouse, and rat whole blood (IC50s = 22, 347, and 91 nM, respectively). It also Inhibits IL-23-induced STAT3 phosphorylation in human CD161+CD3+ Th17 cells (IC50 = 3.7 nM). Zasocitinib (3, 10, and 30 mg/kg twice per day) decreases ankle diameter in a rat model of adjuvant-induced arthritis. It reduces the colon weight-to-length ratio and improves histology scores in a mouse model of colitis induced by an anti-CD40 antibody when administered at doses of 30 and 90 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Leit, S., Greenwood, J., Carriero, S., et al. Discovery of a potent and selective tyrosine kinase 2 inhibitor: TAK-279. J. Med. Chem. 66(15), 10473-10496 (2023).