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Ilorasertib hydrochloride

MCE China：Ilorasertib hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-16018A

CAS：1847485-91-9

Synonyms：ABT-348 hydrochloride

Purity：98.48%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Ilorasertib (ABT-348) hydrochloride 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 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).

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[2]. Ilorasertib hydrochloride (1-1000 nM) shows antiproliferative activity[2].

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[1]. 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[1]. 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[2]. Ilorasertib hydrochloride (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse[2]. Ilorasertib hydrochloride (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse[2].

IC50 & Target：Aurora C 1 nM (IC50) Aurora B 7 nM (IC50) Aurora B (Y156H) 12 nM (IC50) Aurora A 120 nM (IC50) PDGFRα 11 nM (IC50) PDGFRβ 13 nM (IC50) VEGFR1 1 nM (IC50) VEGFR2 2 nM (IC50) VEGFR3 43 nM (IC50) FLT3 1 nM (IC50) CSF-1R 3 nM (IC50) c-KIT 20 nM (IC50)

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References：

[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.  [Content Brief]