GDC-046

Names

[ Name ]:
GDC-046

[Synonym ]:
2,6-Dichloro-N-{2-[(cyclopropylcarbonyl)amino]-4-pyridinyl}benzamide
Benzamide, 2,6-dichloro-N-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-
GDC046

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

[Target]

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].

[References]

[1]. Jun Liang, et al. Lead Optimization of a 4-aminopyridine Benzamide Scaffold to Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
518.0±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₃Cl₂N₃O₂

[ Molecular Weight ]:
350.199

[ Flash Point ]:
267.1±30.1 °C

[ Exact Mass ]:
349.038483

[ PSA ]:
71.09000

[ LogP ]:
3.12

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.721

Related Compounds

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