AMG 900

Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Their expression is elevated in a variety of human cancers. AMG 900 is an orally bioavailable, selective Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively. It is greater than 10-fold selective for Aurora kinases over p38alpha, TYK2, JNK2, Met, and Tie2 (IC50s = 53, 220, 520, 550, and 650 nM, respectively). At 2-3 nM, AMG 900 has been shown to inhibit the proliferation of 26 different tumor cell lines in vitro, including cell lines resistant to either the antimitotic agent paclitaxel (Cay-10461) or to other Aurora kinase inhibitors. Furthermore, AMG 900 is reported to be broadly active in multiple xenograft models, including three multidrug-resistant xenograft models, representing five tumor types.Formal Name: N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine. CAS Number: 945595-80-2. Molecular Formula: C28H21N7OS. Formula Weight: 503.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 15 mg/ml. lambdamax: 212, 325 nm. SMILES: NC1=NC=CC(C2=C(OC3=CC=C(NC4=C(C=CC=C5)C5=C(C6=CC(C)=CS6)N=N4)C=C3)N=CC=C2)=N1. InChi Code: InChI=1S/C28H21N7OS/c1-17-15-24(37-16-17)25-20-5-2-3-6-21(20)26(35-34-25)32-18-8-10-19(11-9-18)36-27-22(7-4-13-30-27)23-12-14-31-28(29)33-23/h2-16H,1H3,(H,32,35)(H2,29,31,33). InChi Key: IVUGFMLRJOCGAS-UHFFFAOYSA-N.