OSU-T315
|
|
|
- CAS号:
- 2070015-22-2
- 英文名:
- ILK-IN-2
- 英文别名:
- ILK-IN-2;OSU-T315 (ILK-IN-1);OSU-T315 (1,3-regioisomer);OSU-T315 (1,5-regioisomer);Inhibitor,Integrin,OSU-T315,OSU-T-315,Apoptosis,inhibit,Autophagy,OSU T315,OSUT315;1H-Pyrazole-5-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-;N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide;N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide
- 中文名:
- OSU-T315
- 中文别名:
- 化合物ILK-IN-2;ILK-IN-2游离态;ILK抑制剂(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;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
- CBNumber:
- CB43121106
- 分子式:
- C30H30F3N5O
- 分子量:
- 533.59
- MOL File:
- 2070015-22-2.mol
|
|
|
OSU-T315化学性质
-
储存条件:
-
2-8°C(protect from light)
-
|
-
溶解度:
-
DMSO: ≥ 50 mg/mL (93.70 mM); Water: < 0.1 mg/mL (insoluble)
-
|
OSU-T315性质、用途与生产工艺
OSU-T315 (ILK-IN-2)是一种有效的 Integrin-Linked Kinase (ILK) 的抑制剂，其IC50值为0.6 μM。OSU-T315 可诱导自噬和细胞凋亡，这两者都是其抗增殖活性不可或缺的。OSU-T315 具有抗肿瘤活性。
| 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).
|
OSU-T315
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-18676B | OSU-T315
ILK-IN-2 | 2070015-22-2 | 2mg | 1200元 |
| 2024/01/25 | HY-18676B | OSU-T315
ILK-IN-2 | 2070015-22-2 | 5mg | 2400元 |
2070015-22-2, OSU-T315 相关搜索:
- 对照品
- 细胞生物学试剂
- 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
- ILK-IN-2游离态
- ILK抑制剂(ILK-IN-2)
- 2070015-22-2
- N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide
- Inhibitor,Integrin,OSU-T315,OSU-T-315,Apoptosis,inhibit,Autophagy,OSU T315,OSUT315
- OSU-T315 (1,5-regioisomer)
- 1H-Pyrazole-5-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-
- OSU-T315 (ILK-IN-1)
- OSU-T315 (1,3-regioisomer)
- N-Methyl-3-(1-(4-(piperazin-1-yl)phenyl)-3-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-5-yl)propanamide
- ILK-IN-2