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CAS No. : 945595-80-2
MCE 国际站:AMG 900
产品活性:AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂,作用于 Aurora A,B 和 C,IC50 分别为 5 nM,4 nM 和 1 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:Aurora Kinase
In Vitro: AMG 900 inhibits the enzyme activity of all 3 aurora kinase family members with IC50 values of 5 nM or less. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B in a concentration-dependent manner. Treatment of HCT116 cells with 50 nM of AMG 900 for 48 hours resulted in polyploidy and suppresses the formation of colonies after cell replating. AMG 900 inhibits cell proliferation, with EC50 values ranging from 0.7 to 5.3 nM. Importantly, 4 of these AMG 900-sensitive cell lines (HCT-15, MES-SA-Dx5, 769P, and SNU449) are resistant to paclitaxel and other anticancer agents. AMG 900 inhibits p-histone H3 or induced polyploidy across all the cell lines tested irrespective of P-gp or BCRP status with uniform potency (IC50 or EC50 values ranging from 2 to 3 nM).
In Vivo: AMG 900 exhibits significant antitumor activity in all 9 xenograft models tested (50%-97% TGI compared with the vehicle-treated control group, P<0.005, P<0.0005). Importantly, AMG 900 is active in the MES-SA-Dx5 (84% TGI, P<0.0001) and NCI-H460-PTX (66% TGI, P<0.0001) xenograft models that are resistant to either Docetaxel or Paclitaxel administered at their respective maximum tolerated doses. AMG 900 inhibits the activity of aurora-B in HCT116 tumors and suppresses the growth of multiple xenografts that represent diverse tumor types. Treatment with AMG 900 at 15 mg/kg significantly inhibits p-Histone H3 in the G2M cell population in mouse bone marrow and cytokeratin positive COLO 205 tumor compared with vehicle-treated controls. AMG 900 exhibits a low-to-moderate clearance and a small volume of distribution. Its terminal elimination half-life ranged from 0.6 to 2.4 h. AMG 900 is well-absorbed in fasted animals with an oral bioavailability of 31% to 107%. Food intake had an effect on rate (rats) or extent (dogs) of AMG 900 oral absorption.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Chemical Probe Library | Anti-Blood Cancer Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | AAPK-25 | AT9283 | Aurora kinase inhibitor-3 | Aurora Kinases-IN-2 | ENMD-2076 Tartrate | Barasertib-HQPA | dAURK-4 | SCH-1473759 | Aurora A inhibitor 1 | BI-847325 | CCT129202 | Tripolin A | ZM-447439 | LY3295668 | TAK-632 | Aurora inhibitor 1 | MK-8745 | Ilorasertib | JB170 | PHA-680632 | Aurora kinase inhibitor-8 | SNS-314 | Hesperadin | Tozasertib | Alisertib | Aurora A/PKC-IN-1 | Derrone | KW-2449
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