ABT-348
- CAS No.
- 1227939-82-3
- Chemical Name:
- ABT-348
- Synonyms
- ABT-348;A-968660;Vilaprisan;A 968660.0;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
- CBNumber:
- CB12627248
- Molecular Formula:
- C25H21FN6O2S
- Molecular Weight:
- 488.54
- MDL Number:
- MFCD25976780
- MOL File:
- 1227939-82-3.mol
| Product description | Number | Pack Size | Price |
| Ilorasertib ≥98.0% | CS-6804 | 50mg | $600 |
| Ilorasertib ≥98.0% | CS-6804 | 100mg | $1100 |
| 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 |
| FDA UNII | 6L5D03D975 |
| NCI Drug Dictionary | ilorasertib |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319-H317-H335 | |||||||||
| Precautionary statements | P261-P264-P271-P272-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P333+P313-P337+P313-P363-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
ABT-348 Chemical Properties,Uses,Production
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)
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
ABT-348 Preparation Products And Raw materials
Raw materials
Preparation Products
ABT-348 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Nanjing Doge Biomedical Technology Co., Ltd | +86-25-58227606 +86-15305155328 | sales@dogechemical.com | China | 4128 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 43339 | 58 |
| Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39002 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
| ROSEWA HOLDING GROUP CO.,LIMITED | +86-023-62871537 | sales@rosewachem.com | China | 2803 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2922 | 55 | |
| Wuhan ariel chemical Co., LTD. | 18986259541 | sales@3stc.com | China | 3764 | 58 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1493 | 55 |
