N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Basic information
- Product Name:
- N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
- Synonyms:
-
- N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide
- ILK-IN-1
- BDBM50353484
- CHEMBL1830587
- CS-4936
- GTPL8116
- SCHEMBL8536228
- OSU-T315
- CAS:
- 1333146-24-9
- MF:
- C30H30F3N5O
- MW:
- 533.59
- Mol File:
- 1333146-24-9.mol
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Chemical Properties
- Boiling point:
- 739.2±60.0 °C(Predicted)
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 10mM
- form
- A solid
- pka
- 16.02±0.46(Predicted)
- color
- White to light yellow
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide Usage And Synthesis
Uses
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models[1][2].
in vivo
ILK-IN-2 (25-50 mg/kg, oral or intraperitoneal injection, once daily, 2-4 weeks) delays leukemia progression in mice and significantly improves the overall survival rate of mice harboring TCL1 leukemia cells[ 1 ].
ILK-IN-2 (25-50 mg/kg, orally, daily, for 35 days) inhibits the growth of PC-3 xenograft tumors in nude mice[2].
| Animal Model: | Pharmacokinetic properties of OSU-T315[1] |
| Dosage: | 50 mg/kg, daily for 4 weeks; 25 mg/kg, once daily for 2 weeks |
| Administration: | Oral; Intraperitoneal injection (i.p.) |
| Result: | Reduced white blood cell count and prolonged the survival of mice. |
| Animal Model: | PC-3 tumor xenograft mice model[2] |
| Dosage: | 25, 50 mg/kg; daily; 35 days |
| Administration: | Oral |
| Result: | Significantly inhibited tumor growth (25 and 50 mg/kg groups inhibited 48% and 62% respectively). Showed that the phosphorylation of Ser-473-Akt was dose-dependently inhibited, while the phosphorylation of Thr-308-Akt was not affected. At the same time, the phosphorylation levels of GSK3β and MLC and the expression levels of YB-1, HER2 and EGFR also appeared in parallel decline. |
IC 50
ILK: 0.6 μM (IC50)
References
[1] Ta-Ming Liu, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. DOI:10.1182/blood-2014-06-583518
[2] Su-Lin Lee, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. DOI:10.1021/jm2007744
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