OSU-T315
中文名称 | OSU-T315 |
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中文同义词 | ILK抑制剂(ILK-IN-2);ILK-IN-2游离态;N-甲基-3-(1-(4-(哌嗪-1-基)苯基)-3-(4'-(三氟甲基)-[1,1'-联苯基]-4-基)-1H-吡唑-5-基)丙胺;化合物ILK-IN-2;N-甲基-3-(1-(4-(哌嗪-1-基)苯基)-3-(4'-(三氟甲基)-[1,1'-联苯基]-4-基)-1H-吡唑-5-基)丙胺 |
英文名称 | ILK-IN-2 |
英文同义词 | ILK-IN-2;N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide;OSU-T315 (1,3-regioisomer);OSU-T315 (ILK-IN-1);1H-Pyrazole-5-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-;OSU-T315 (1,5-regioisomer);Inhibitor,Integrin,OSU-T315,OSU-T-315,Apoptosis,inhibit,Autophagy,OSU T315,OSUT315;N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide |
CAS号 | 2070015-22-2 |
分子式 | C30H30F3N5O |
分子量 | 533.59 |
EINECS号 | |
相关类别 | 细胞生物学试剂;对照品 |
Mol文件 | 2070015-22-2.mol |
结构式 |
OSU-T315 性质
储存条件 | 2-8°C(protect from light) |
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溶解度 | DMSO:≥50mg/mL(93.70mM);水:< 0.1 mg/mL(不溶) |
Target | Value |
ILK
(Cell-free assay) | 0.6 μM |
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 IC
50
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), 1-2.5μM). |
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. |
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). |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-18676B | OSU-T315 ILK-IN-2 | 2070015-22-2 | 2mg | 1200元 |
2024/04/30 | S6840 | OSU-T315 OSU-T315 | 2070015-22-2 | 2mg | 2148.64元 |