OSU-T315 (15-regioisomer)

SKU: orb1220931

Description

OSU-T315 (15-regioisomer) is a ILK inhibitor.

Key Properties

• CAS Number: 2070015-22-2
• MW: 533.6
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₀F₃N₅O
• SMILES: CNC(=O)CCc1cc(nn1-c1ccc(cc1)N1CCNCC1)-c1ccc(cc1)-c1ccc(cc1)C(F)(F)F
• Target: Integrin
• Solubility: DMSO:50 mg/mL (93.70 mM)

Bioactivity

• In Vivo:
  OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth. No other obvious toxicity is observed in mice. 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. Result: 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).
• In Vitro:
  OSU-T315 (Compound 22; 0-5 μM; 24 hours) exhibits high in vitro potency against a panel of prostate and breast cancer cell lines with a IC50 range of 1-2.5 μM. OSU-T315 (0-2.5 μM; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressive effect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell. OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition. Western blot analysis. Cell line: PC-3 cells; MDA-MB-231 cells. Concentration: 1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM Incubation time: 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. Cell Viability Assay Cell line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells. Concentration: 0-5 μM. Incubation time: 24 hours. Result: Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5 μM). Apoptosis Analysis. Cell line: PC-3 cells. Concentration: 1 μM, 2 μM, 3 μM, 4 μM. Incubation time: 24 hours. Result: Induced accumulation of LC3-II and PARP cleavage.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ILK-IN-2

Quick Database Links

Gene Symbol

Integrin