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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1889279-16-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3895.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1100.0 |
| 规格： | 5 mg | 产品价格： | ￥3300.0 |
| 规格： | 10 mg | 产品价格： | ￥5000.0 |
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A-485
CAS No. : 1889279-16-6
MCE 国际站：A-485
产品活性：A-485 是 p300/CBP 的强效选择性催化抑制剂，对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC50 值分别为 9.8 nM 和 2.6 nM。
研究领域：Epigenetics
作用靶点：Epigenetic Reader Domain | Histone Acetyltransferase
In Vitro: A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC50) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.
The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines.
In Vivo: After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen.
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