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ILK-IN-2 (OSU-T315) is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $40 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $130 | In Stock | |
25 mg | $165 | In Stock | |
50 mg | $203 | In Stock | |
100 mg | $296 | In Stock | |
200 mg | $429 | In Stock | |
1 mL x 10 mM (in DMSO) | $139 | In Stock |
Description | ILK-IN-2 (OSU-T315) is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM. |
In vitro | ILK-IN-25 exhibited high in vitro potency against a panel of prostate and breast cancer cell lines (IC(50), 1-2.5 μM), while normal epithelial cells were unaffected. ILK-IN-25 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including glycogen synthase kinase-3β and myosin light chain. Moreover, ILK-IN-25 suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells, which could be rescued by the stable expression of constitutively active ILK [1]. The cytotoxicity of ILK-IN-25 in normal B or T cells was significantly lower (LC50 > 10 μM). ILK-IN-25 had the effect of dose-dependent cytotoxicity toward 2 CLL-derived cell lines, Mec-1 and OSU-CLL (LC50 of 2-3 μM in both) after 24-hour treatment [2]. |
In vivo | Athymic nude mice bearing established subcutaneous PC-3 tumors were treated with oral ILK-IN-25 once daily at 25 and 50 mg/kg or vehicle control. The daily administration of ILK-IN-25 at both doses was well tolerated. Treatment with oral ILK-IN-25 in either dose resulted in significant 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) [1]. |
Alias | OSU-T315 |
Molecular Weight | 533.59 |
Formula | C30H30F3N5O |
Cas No. | 1333146-24-9 |
Smiles | CNC(=O)CCc1cc(-c2ccc(cc2)-c2ccc(cc2)C(F)(F)F)n(n1)-c1ccc(cc1)N1CCNCC1 |
Relative Density. | 1.27 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 9 mg/mL (16.87 mM), Sonication is recommended. ![]() | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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