Name | 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide |
---|---|
Synonyms |
2,6-Dichloro-N-{2-[(cyclopropylcarbonyl)amino]-4-pyridinyl}benzamide
Benzamide, 2,6-dichloro-N-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]- GDC046 |
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 |
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 |