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编 号：F083037
分子式：C25H21FN6O2S
分子量：488.54
分子式：C25H21FN6O2S
分子量：488.54
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CAS No: 1227939-82-3
产品详情
生物活性：
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
体内研究：
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.Animal Model:Female SCID/beige mice
Dosage:25 mg/kg
Administration:Subcutaneous minipump; 24 h
Result:Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.
Animal Model:22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))
Dosage:20 mg/kg
Administration:P.o.; once weekly for 3 weeks
Result:Inhibited the tumor growth in mouse.
体外研究：
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.
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
体内研究：
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.Animal Model:Female SCID/beige mice
Dosage:25 mg/kg
Administration:Subcutaneous minipump; 24 h
Result:Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.
Animal Model:22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))
Dosage:20 mg/kg
Administration:P.o.; once weekly for 3 weeks
Result:Inhibited the tumor growth in mouse.
体外研究：
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.
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