2070015-22-2
2070015-22-2 結(jié)構(gòu)式
基本信息
ILK抑制劑(ILK-IN-2)
OSU-T315 (ILK-IN-1)
OSU-T315 (1,3-regioisomer)
OSU-T315 (1,5-regioisomer)
1H-Pyrazole-5-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | HY-18676B | OSU-T315 ILK-IN-2 | 2070015-22-2 | 2mg | 1200元 |
| 2024/11/08 | HY-18676B | OSU-T315 ILK-IN-2 | 2070015-22-2 | 5mg | 2400元 |
| 2024/11/08 | HY-18676B | OSU-T315 ILK-IN-2 | 2070015-22-2 | 10mM * 1mLin DMSO | 2817元 |
常見(jiàn)問(wèn)題列表
| 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). |