AMG 548

AMG 548 - Names and Identifiers

Name	2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone dihydrochloride
Synonyms	AMG-548 AMG 548 AMG-548(AMG548) AMG-548 dihydrochloride 2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone 4(3H)-Pyrimidinone, 2-[[(2S)-2-amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)- 2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone dihydrochloride
CAS	864249-60-5

AMG 548 - Physico-chemical Properties

Molecular Formula	C29H27N5O
Molar Mass	461.56
Solubility	DMSO: soluble5mg/mL, clear (warmed)
Appearance	powder
Color	white to beige
Storage Condition	-20°C
In vitro study	AMG-548 shows >1000 fold selective against p38γ (K i =2600 nM) and p38δ (k i =4100 nM). AMG-548 has an modest selectivity against JNK2 (k i =39 nM) and JNK3 (k i =61 nM). AMG-548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC 50 =3 nM) and IL1b (IC 50 =7 nM) as well as TNFa induced IL-8 (IC 50 =0.7 nM) and IL-1b induced IL-6 (IC50 50 =1.3 nM) in human whole blood. AMG-548 (10 μM) inhibits the hDvl2 shift.
In vivo study	AMG-548 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.

AMG 548 - Risk and Safety

Hazard Symbols	T - Toxic
Risk Codes	R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin.
Safety Description	S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.)
UN IDs	UN 2811 6.1 / PGIII
WGK Germany	3

AMG 548 - References

biological activity

AMG-548 is an orally effective, selective p38α inhibitor (Ki = 0.5 nM), there was slight selectivity for p38β (Ki = 36 nM) and> 1000-fold selectivity for p38γ and p38δ. AMG 548 also potently inhibited LPS-stimulated TNFα in whole blood (IC50=3 nM). AMG-548 inhibition of Wnt signaling by direct inhibition of Casein kinase 1 isoforms Delta and Epsilon.

Last Update：2024-04-09 21:54:55