OSU-T315 |
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カタログ番号GC36821
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OSU-T315 (ILK-IN-1) は、IC50 が 0.6 μM の小さなインテグリン結合キナーゼ (ILK) 阻害剤であり、AKT-Ser473 および他の ILK 標的 (GSK-3β およびミオシン光) の脱リン酸化によって PI3K/AKT シグナル伝達を阻害します。鎖)。 OSU-T315 は、脂質ラフトでの AKT の局在化を阻害することで AKT の活性化を無効にし、ILK に依存しない方法でカスパーゼ依存性のアポトーシスを引き起こします。 OSU-T315 は、アポトーシスとオートファジーによって細胞死を引き起こします。
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Cas No.: 2070015-22-2
Sample solution is provided at 25 µL, 10mM.
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain)[1]. OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner[2]. OSU-T315 causes cell death through apoptosis and autophagy[1]. IC50: 0.6μM; Integrin-linked kinase (ILK) inhibitor[1]
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[1].OSU-T315 (0-4 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[1]. OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition[1]. Cell Viability Assay [1] Cell Line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells
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 [1]. No other obvious toxicity is observed in mice[1]. Animal Model: Male NCr athymic nude mice with PC-3 tumor xenografts
[1]. Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18): 6364-6374 [2]. Liu TM, 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.
| Cas No. | 2070015-22-2 | SDF | |
| Canonical SMILES | O=C(NC)CCC1=CC(C2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)=NN1C4=CC=C(N5CCNCC5)C=C4 | ||
| Formula | C30H30F3N5O | M.Wt | 533.59 |
| 溶解度 | DMSO: ≥ 50 mg/mL (93.70 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8741 mL | 9.3705 mL | 18.741 mL |
| 5 mM | 374.8 μL | 1.8741 mL | 3.7482 mL |
| 10 mM | 187.4 μL | 937 μL | 1.8741 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)















