A JAK1 and JAK3 inhibitor
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Lepzacitinib

Item No. 44278

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(3R)-1-(2-cyanoacetyl)-3-piperidinyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid, ethyl ester
CAS Number
2321488-47-3
Synonyms
  • ATI-1777
Molecular Formula
C18H21N5O3
Formula Weight
355.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CCOC(C1=CN=C(NC=C2)C2=C1N[C@H]3CN(CCC3)C(CC#N)=O)=O
InChi Code
InChI=1S/C18H21N5O3/c1-2-26-18(25)14-10-21-17-13(6-8-20-17)16(14)22-12-4-3-9-23(11-12)15(24)5-7-19/h6,8,10,12H,2-5,9,11H2,1H3,(H2,20,21,22)/t12-/m1/s1
InChi Key
QQOPOYMFJLUSBI-GFCCVEGCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $124

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    10 mg

    $201

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    25 mg

    $385

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    Product Description

    Lepzacitinib is an inhibitor of JAK1 and JAK3 (IC50s = 1.5 and 3.6 nM, respectively).1 It selectively inhibits IL-2-induced activation of JAK1/3 over IFN-γ-induced activation of JAK1/2, GM-CSF-induced activation of JAK2, and IL-12-induced activation of JAK2/tyrosine kinase 2 (TYK2) in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 19, 97, 794, and 898 nM, respectively). Lepzacitinib is also selective for JAK1 and JAK3 over a panel of 214 additional kinases at 1 µM. Topical application of lepzacitinib (2% solution) inhibits IL-15-induced expression of mRNA encoding chemokine (C-C-motif) ligand 8 (CCL8) by 83% in a porcine model of atopic dermatitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Changelian, P., Xu, C., Mnich, S., et al. ATI-1777, a topical Jak1/3 inhibitor, may benefit atopic dermatitis without systemic drug exposure: Results from preclinical development and phase 2a randomized control study ATI-1777-AD-201. JID Innov. 4(2), 100251 (2023).