A TYK2 inhibitor
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GDC-046

Item No. 36601

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,6-dichloro-N-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-benzamide
CAS Number
1258292-64-6
Molecular Formula
C16H13Cl2N3O2
Formula Weight
350.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
242 nm
SMILES
O=C(C1=C(Cl)C=CC=C1Cl)NC2=CC=NC(NC(C3CC3)=O)=C2
InChi Code
InChI=1S/C16H13Cl2N3O2/c17-11-2-1-3-12(18)14(11)16(23)20-10-6-7-19-13(8-10)21-15(22)9-4-5-9/h1-3,6-9H,4-5H2,(H2,19,20,21,22,23)
InChi Key
IAFNAEGXTKTGHN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $163

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    10 mg

    $304

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    25 mg

    $433

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    Product Description

    GDC-046 is a tyrosine kinase 2 (TYK2) inhibitor (Ki = 4.8 nM).1 It is selective for TYK2 over JAK1, -2, and -3 (Kis = 83.8, 27.6, and 253 nM, respectively). GDC-046 selectively inhibits TYK2-mediated IL-12-induced phosphorylation of STAT4 over JAK1-mediated IL-6-induced phosphorylation of STAT3 and JAK2-mediated erythropoietin-induced phosphorylation of STAT5 in cell-based assays (EC50s = 380, 2,000, and 1,700 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liang, J., van Abbema, A., Balazs, M., et al. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. J. Med. Chem. 56(11), 4521-4536 (2013).