AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM).

AMG-548 hydrochloride has a modest selectivity against JNK2 (Ki: 39 nM) and JNK3 (Ki: 61 nM). It is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC50: 3 nM) and IL1b (IC50: 7 nM) as well as TNFa induced IL-8 (IC50: 0.7 nM) and IL-1b induced IL-6 (IC50: 1.3 nM) in human whole blood [1]. AMG-548 hydrochloride (10 μM) inhibits the hDvl2 shift [2].

AMG-548 hydrochloride has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs [1].

T10298

C29H28ClN5O

498.02

AMG-548 hydrochloride;AMG-548 hydrochloride (864249-60-5 free base)

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years