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AMG 900 is a potent and highly selective pan-aurora kinase inhibitor with IC50 values of 5, 4 and 1 nM for Aurora A, B and C respectively. AMG 900 inhibited autophosphorylation of aurora-A and -B as well as phosphorylation of histone H3 on Ser(10) in tumor cells. AMG 900 exhibited acceptable PK properties in preclinical species and was predicted to have low clearance in humans. Oral administration of AMG 900 blocked the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibited the growth of HCT116 tumor xenografts. Importantly, AMG 900 was broadly active in multiple xenograft models, including 3 multidrug-resistant xenograft models, representing 5 tumor types. AMG 900 is currently in Phase I clinical testing as a treatment for solid tumours.
| Molecular Weight | 503.58 |
| Formula | C28H21N7OS |
| CAS Number | 945595-80-2 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Aurora Kinase Products |
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| Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. |
| Aurora Kinases-IN-4
Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). |
| Derrone
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. |
| CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
| Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
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