1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. GDC-046

GDC-046 

Cat. No.: HY-120469
Handling Instructions

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

For research use only. We do not sell to patients.

GDC-046 Chemical Structure

GDC-046 Chemical Structure

CAS No. : 1258292-64-6

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Description

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively[1].

IC50 & Target[1]

Tyk2

4.8 nM (Ki)

JAK1

0.7 nM (Ki)

JAK2

0.7 nM (Ki)

JAK3

0.4 nM (Ki)

In Vitro

In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM)[1].

In Vivo

In mice, GDC-046 exhibits relatively high clearance (65 mL/min/kg) when dosed intravenously (i.v. 1 mg/kg) and exhibits modest oral exposure (AUC=2.6 μM·h at p.o. 5 mg/kg)[1].

Molecular Weight

350.20

Formula

C₁₆H₁₃Cl₂N₃O₂

CAS No.

1258292-64-6

SMILES

O=C(NC1=CC(NC(C2CC2)=O)=NC=C1)C3=C(Cl)C=CC=C3Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GDC-046GDC046GDC 046JAKJanus kinaseinflammatoryboweldiseasesIBDIL-23IL-12TYK2JAK1JAK2JAK3Inhibitorinhibitorinhibit

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