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CAS No. : 1847485-91-9
MCE 国际站:Ilorasertib hydrochloride
产品活性:Ilorasertib (ABT-348) hydrochloride 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 hydrochloride 也是一种有效的 VEGF 和 PDGF 抑制剂。Ilorasertib hydrochloride 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 | PDGFR | VEGFR
In Vitro: Ilorasertib hydrochloride (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells.
Ilorasertib hydrochloride (1-1000 nM) shows antiproliferative activity.
In Vivo: Ilorasertib hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse.
Ilorasertib hydrochloride (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse.
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