Name | ILK-IN-2 |
Synonyms | OSU-T315 ILK-IN-2 OSU-T315 (ILK-IN-1) OSU-T315 (1,3-regioisomer) OSU-T315 (1,5-regioisomer) 1H-Pyrazole-5-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]- N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide |
CAS | 2070015-22-2 |
Molecular Formula | C30H30F3N5O |
Molar Mass | 533.59 |
Solubility | DMSO : 50 mg/mL (93.70 mM);H2O : < 0.1 mg/mL (insoluble) |
Storage Condition | 2-8°C(protect from light) |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.874 ml | 9.37 ml | 18.741 ml |
5 mM | 0.375 ml | 1.874 ml | 3.748 ml |
10 mM | 0.187 ml | 0.937 ml | 1.874 ml |
5 mM | 0.037 ml | 0.187 ml | 0.375 ml |
biological activity | OSU-T315 (ILK-IN-2) is a potent inhibitor of Integrin-Linked Kinase (ILK), the IC50 value was 0.6 μm. OSU-T315 induces autophagy and apoptosis, both of which are essential for its antiproliferative activity. OSU-T315 has anti-tumor activity. |
Target | Value |
ILK (Cell-free assay) | 0.6 μM |
Cell Line: | PC-3 cells; MDA-MB-231 cells Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells PC-3 cells |
Concentration: | 1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM 0-5 μM 1 μM, 2 μM, 3 μM, 4 μM |
Incubation Time: | 24 hours 24 hours 24 hours |
Result: | Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, and p38 in PC-3 cells and MDA-MB-231 cells. Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5μM). Induced accumulation of LC3-II and PARP cleavage. Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively). |
Animal Model: | Male NCr athymic nude mice with PC-3 tumor xenografts |
Dosage: | 25 mg/kg; 50 mg/kg |
Administration: | Oral gavage; single daily; 35 days |