| Identification | Back Directory | [Name]
2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide | [CAS]
1258292-64-6 | [Synonyms]
GDC-046
GDC-046;GDC 046
2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
Benzamide, 2,6-dichloro-N-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]- | [Molecular Formula]
C16H13Cl2N3O2 | [MDL Number]
MFCD28155087 | [MOL File]
1258292-64-6.mol | [Molecular Weight]
350.2 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 62.5 mg/mL (178.47 mM; Need ultrasonic) | [form ]
A solid | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [IC 50]
Tyk2: 4.8 nM (Ki); JAK1: 0.7 nM (Ki); JAK2: 0.7 nM (Ki); JAK3: 0.4 nM (Ki) | [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. DOI:10.1021/jm400266t |
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