GDC-046

Modify Date: 2024-01-10 12:42:15

GDC-046 Structure
GDC-046 structure
Common Name GDC-046
CAS Number 1258292-64-6 Molecular Weight 350.199
Density 1.5±0.1 g/cm3 Boiling Point 518.0±50.0 °C at 760 mmHg
Molecular Formula C16H13Cl2N3O2 Melting Point N/A
MSDS N/A Flash Point 267.1±30.1 °C

 Use of GDC-046


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].

 Names

Name 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
Synonym More Synonyms

 GDC-046 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
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

 Synonyms

2,6-Dichloro-N-{2-[(cyclopropylcarbonyl)amino]-4-pyridinyl}benzamide
Benzamide, 2,6-dichloro-N-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-
GDC046
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: GDC046
  • Price: $650.0/100mg $1200.0/250mg $2500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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