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2070015-22-2

中文名稱(chēng) OSU-T315
英文名稱(chēng) ILK-IN-2
CAS 2070015-22-2
分子式 C30H30F3N5O
分子量 533.59
MOL 文件 2070015-22-2.mol
更新日期 2024/11/08 11:24:23
2070015-22-2 結(jié)構(gòu)式 2070015-22-2 結(jié)構(gòu)式

基本信息

中文別名
ILK-IN-2游離態(tài)
ILK抑制劑(ILK-IN-2)
英文別名
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)

儲(chǔ)存條件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO: ≥ 50 mg/mL (93.70 mM); Water: < 0.1 mg/mL (insoluble)
形態(tài)Solid
顏色White to off-white
OSU-T315價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-18676BOSU-T315
ILK-IN-2
2070015-22-22mg1200元
2024/11/08HY-18676BOSU-T315
ILK-IN-2
2070015-22-25mg2400元
2024/11/08HY-18676BOSU-T315
ILK-IN-2
2070015-22-210mM * 1mLin DMSO2817元

常見(jiàn)問(wèn)題列表

生物活性
OSU-T315 (ILK-IN-2)是一種有效的 Integrin-Linked Kinase (ILK) 的抑制劑,其IC50值為0.6 μM。OSU-T315 可誘導(dǎo)自噬和細(xì)胞凋亡,這兩者都是其抗增殖活性不可或缺的。OSU-T315 具有抗腫瘤活性。
靶點(diǎn)
TargetValue
ILK
(Cell-free assay)
0.6 μM
體外研究

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.
體內(nèi)研究

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).
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