Ilorasertib,1227939-82-3

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Ilorasertib

CAS No. : 1227939-82-3

MCE 国际站：Ilorasertib

产品活性：Ilorasertib (ABT-348) 是一种有效的，具有口服活性和 ATP 竞争性的 aurora 抑制剂，对 aurora A, aurora B, aurora C 的 IC₅₀ 值分别为 116, 5, 1 nM。Ilorasertib 也是一种有效的 VEGF 和 PDGF 抑制剂。Ilorasertib 具有用于急性髓系白血病 (AML) 和骨髓增生异常综合征 (MDS) 的研究潜力。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Protein Tyrosine Kinase/RTK

作用靶点：Aurora Kinase  |  VEGFR  |  PDGFR

In Vitro: Ilorasertib (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells.
Ilorasertib (1-1000 nM) shows antiproliferative activity.

In Vivo: Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in MV-4-11 tumor-bearing SCID mice with TGI of 80%, 86%, 94% at 6.25, 12.5, 25 mg/kg, respectively.
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively.
Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells.
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse.
Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse.

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