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。

Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC 50 s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

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Aurora C 1 nM (IC50) Aurora B 7 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay-tbl">

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Yi-Chun Wang, et al. Abstract 858: Potent in vivo activity of the aurora kinase inhibitor ABT-348 in human acute myeloid leukemia and myelodysplastic syndrome xenograft models. Cancer Res (2012) 72 (8_Supplement): 858.
[2]. Glaser KB, et al. Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.

In Vitro: DMSO : 41.67 mg/mL (79.37 mM; Need ultrasonic)配制储备液