AMG-548 dihydrochloride

AMG-548 dihydrochloride, an orally active and selective p38α inhibitor ( K i =0.5 nM), shows slightly selective over p38β ( K i =36 nM) and >1000 fold selective against p38γ and p38δ . AMG-548 dihydrochloride is also extremely potent in the inhibition of IC50& Target:p38α|0.5 nM (Ki)|p38β|3.6 nM (Ki)|p38δ|2600 nM (Ki)|p38γ|4100 nM (Ki)|dog p38α|5.0 nM (Ki)|JNK 1|11480 nM (Ki)|JNK 2|39 nM (Ki)|JNK 3|61 nM (Ki)|CK1 In Vitro:AMG-548 dihydrochloride shows >1000 fold selective against p38γ (K i =2600 nM) and p38δ (k i =4100 nM). AMG-548 dihydrochloride has an modest selectivity against JNK2 (k i =39 nM) and JNK3 (k i =61 nM). AMG-548 dihydrochloride is also extremely potent in In Vivo:AMG-548 dihydrochloride has rat F of 62% and dog F of 47%. The t 1/2 is 4.6 hours in rats and 7.3 hours in dogs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Biological Activity:AMG-548 dihydrochloride, an orally active and selective p38α inhibitor ( K i =0.5 nM), shows slightly selective over p38β ( K i =36 nM) and >1000 fold selective against p38γ and p38δ . AMG-548 dihydrochloride is also extremely potent in the inhibition of

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