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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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| AT9283
AT9283 is a potent inhibitor of several protein kinases, including Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL. |
| AZD1152-HQPA
AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora B and Aurora A respectively. |
| CCT-129202
CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. |
| CYC116
CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. |
| ENMD-2076
ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor. |
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