Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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OSU-T315 (ILK-IN-1) is a novel, potent and specific small molecule inhibitor of Integrin-linked kinase (ILK) with an IC50 of 0.6 μM, suppressing cancer cell proliferation in vitro and in vivo and inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
ln Vitro |
Compound 22, OSU-T315 (IC50 ranging from 1-2.5 μM), demonstrates excellent potency in vitro against a panel of prostate and breast cancer cell lines [1]. The expression of YB-1, HER2, and EGFR can be decreased by OSU-T315 (0-2.5 μM; 24 hours); it also exhibits a dose-dependent influence on phosphorylated p38 and ERK1/2 and a modest inhibitory effect on phosphorylated S6 levels. sexual inhibition, whereas PC-3 cells show no change in phosphorylated JNK [1]. ILK inhibition is used by OSU-T315 (0–4 μM; 24 hours) to promote autophagy [1].
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ln Vivo |
PC-3 xenograft tumor growth is inhibited by OSU-T315 (oral gavage; 25 mg/kg, 50 mg/kg; once daily; 35 days) [1]. ?In mice, no additional noteworthy harm was noted [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: PC-3 cells; MDA-MB-231 cells Tested Concentrations: 1μM, 2μM, 3μM, 4μM; 0.5μM, 1μM, 1.5μM, 2μM, 2.5μM Incubation Duration: 24 hrs (hours) Experimental Results: Exhibits a dose-dependent reduction in the phosphorylation of pS6, ERK and p38 in PC-3 cells and MDA-MB-231 cells. Cell viability assay[1] Cell Types: Prostate cancer cells: LNCaP, PC-3; Breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cell Tested Concentrations: 0-5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cancer cell viability in breast and prostate cancer cells (IC (50), 1-2.5 μM). Apoptosis analysis[1] Cell Types: PC-3 Cell Tested Concentrations: 1 μM, 2 μM, 3 μM, 4 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of accumulation of LC3-II and PARP cleavage. |
Animal Protocol |
Animal/Disease Models: Male NCr athymic nude mice with PC-3 tumor xenografts
Doses: 25 mg/kg; 50 mg/kg Route of Administration: po (oral gavage); daily single; 35 days Experimental Results: After 35 days of treatment, relative Tumor growth was inhibited compared to vehicle control (48% and 62% inhibition at 25 mg/kg and 50 mg/kg, respectively). |
References |
[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. |
Molecular Formula |
C₃₀H₃₀F₃N₅O
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Molecular Weight |
533.59
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CAS # |
2070015-22-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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
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Synonyms |
OSUT315 OSU T315 OSU-T315
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 260 mg/mL (~487.27 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8741 mL | 9.3705 mL | 18.7410 mL | |
5 mM | 0.3748 mL | 1.8741 mL | 3.7482 mL | |
10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.