| Identification | Back Directory | [Name]
Ilorasertib hydrochloride | [CAS]
1847485-91-9 | [Synonyms]
ABT-348 hydrochloride
Ilorasertib hydrochloride
ILORASERTIB HYDROCHLORIDE (ABT-348 HYDROCHLORIDE) | [Molecular Formula]
C25H22ClFN6O2S | [MDL Number]
MFCD32201158 | [MOL File]
1847485-91-9.mol | [Molecular Weight]
525 |
| Hazard Information | Back Directory | [Description]
Ilorasertib hydrochloride (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively[1]. | [Uses]
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)[1][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]. | Animal Model: | Female SCID/beige mice[2] | | 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))[2] | | Dosage: | 20 mg/kg | | Administration: | P.o.; once weekly for 3 weeks | | Result: | Inhibited the tumor growth in mouse. |
| [IC 50]
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) | [References]
[1]. 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. |
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