2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Chemical Properties

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

2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Usage And Synthesis

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

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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