| Identification | Back Directory | [Name]
ABT-348 | [CAS]
1227939-82-3 | [Synonyms]
ABT-348
A 968660.0
Vilaprisan
Ilorasertib
Abbott 968660
ILORASERTIB (ABT-348)
N-[4-[4-Amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-N'-(3-fluorophenyl)urea
Urea, N-[4-[4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl]phenyl]-N'-(3-fluorophenyl)-
anti-tumor,H1299,Platelet-derived growth factor receptor,Inhibitor,ABT 348,antiproliferative activity,AML,VEGFR,Ilorasertib,histone H3 phosphorylation,ABT348,Vascular endothelial growth factor receptor,PDGFR,Aurora Kinase,inhibit,H460 cells,MDS | [Molecular Formula]
C25H21FN6O2S | [MDL Number]
MFCD25976780 | [MOL File]
1227939-82-3.mol | [Molecular Weight]
488.54 |
| Chemical Properties | Back Directory | [Boiling point ]
675.7±55.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol: soluble | [form ]
A solid | [pka]
13.56±0.70(Predicted) | [color ]
Off-white to brown |
| Hazard Information | Back Directory | [Uses]
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)[1][2]. | [in vivo]
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[1].
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[1].
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[2].
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse[2].
Ilorasertib (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) | [storage]
Store at -20°C | [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. DOI:10.1124/jpet.112.197087 |
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| Company Name: |
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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SPIRO PHARMA
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| Tel: |
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www.spiropharma.com.cn |
| Company Name: |
Wuhan Topule
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+86-02787215551 19945035818 |
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http://www.topule.com/ |
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