| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
Cell experiment: | Human neuroblastoma SHEP-1 cells are maintained in DMEM supplemented with 10% fetal bovine serum and 1% Penicillin. In a typical survival assay, SHEP-1 cells (8×104 per well) plated in 24-well plates for 24 h are exposed to LY303511 (12.5, 25, and 50 μM), TRAIL (25, 50, and 100 ng/mL), and a combination of the two (1 h preincubation with LY303511 followed by TRAIL for 4 h). Cytotoxicity is determined by the crystal violet assay. After drug exposure, cells are washed with PBS and incubated for 20 min with crystal violet solution (200 μL). The excess crystal violet solution is washed away with distilled water, and the remaining crystals are dissolved with 20% acetic acid. Viability is determined by absorbance at 595 nm wavelength using an automated ELISA reader. Cell viability experiments are performed similarly with 2,000 units/mL of catalase, 4 μM JNK inhibitor SP600125, 10 μM p38 inhibitor SB202190, 20 μM MAPK/ERK kinase (MEK) inhibitor PD98059, 50 μM of caspase-8 inhibitor Z-IETD-FMK or pan-caspase inhibitor Z-VAD-FMK, or death receptor blocking antibodies (4 μg/mL anti-DR4 or 1 μg/mL anti-DR5), or in cells transfected with small interfering RNA (siRNA) for silencing JNK and ERK expression, respectively. Cells are preincubated for 1 h with LY303511 and the respective inhibitor or catalase before the addition of TRAIL. Similar sensitizing effect of LY303511 on TRAIL-induced apoptosis is carried out with SY5Y neuroblastoma, T98G glioblastoma, Jurkat leukemia, CEM myelogenous leukemia, HeLa ovarian carcinoma, and HT29 colorectal carcinoma cell lines[2]. |
Animal experiment: | Mice[4]Human prostate adenocarcinoma (PC-3) cells (ATCC CRL-1435) are cultured in vitro before harvesting and implantation of 1×106 cells in 20% Matrigel per athymic NCR nude mouse by subcutaneous injection at the flank. Inoculated mice are subdivided into four groups of 10. Administration of vehicle or LY303511, 10 mg/kg/day, is begun (day 1) when tumors reach ~150 mm3 (n=35), and tumor volumes are measured for 30 days at the indicated time points. |
| 产品描述 | Description: IC50 Value:N/A LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. in vitro: 100 μM LY303511 significantly reduced the fraction of cells in S phase. The proportion of cells in G2/M remained unchanged, indicating that cells were arrested in both G1 and G2/M. In contrast, rapamycin increased the G1 population by reducing the proportion of cells in both S and G2/M. The effects of 10 μM LY303511 and rapamycin on the reduction in S phase cells were additive to that of 10 μM LY303511 alone (P = 0.056) [1]. In MIN6 insulinoma cells, wortmannin (100 nM) had no effect on whole-cell outward K+ currents, but LY294002 and LY303511 reversibly blocked currents in a dose-dependent manner (IC50=9.0+/-0.7 microM and 64.6+/-9.1 microM, respectively). Western blotting confirmed the specific inhibitory effects of LY294002 and wortmannin on insulin-stimulated PI3K activity [2]. Both LY294002 and LY303511 increased the activity of protein kinase A (PKA). Moreover, PKA blockade by the small molecule inhibitor H89 decreased the LY294002/LY303511-mediated increase in GJIC [3]. in vivo: PND4 ovaries were cultured for 8 days in control medium or medium containing VCD (30 μM) in the presence or absence of LY303511 (20 μM). Incubation with LY303511 alone caused a reduction (P < 0.05) in primordial and small primary follicle numbers. On the other hand, whereas VCD alone depleted (P < 0.05) primordial and small primary follicle numbers, this depletion was not prevented by co-incubation with LY303511 [4]. Clinical trial: N/A |
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