A-485 - CAS:1889279-16-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	A-485 促销
英文名称:	A-485
CAS No:	1889279-16-6	分子式:	C₂₅H₂₄F₄N₄O₅	分子量:	536.48
CAS No:	1889279-16-6
分子式:	C₂₅H₂₄F₄N₄O₅
分子量:	536.48

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A11398 A-485 ≥98% (psaitong)

相关产品

包装规格：

100mg in glass bottle

溶解性：

溶于DMSO（≥220mg/mL）

产品描述：

基本信息

产品编号：A11398
产品名称：A-485
CAS:	1889279-16-6	储存条件	粉末	-20℃	四年

分子式：	C25H24F4N4O5		溶于液体	-80℃	六个月
分子量：	536.48			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	100mg/mL (186.4mM)
		Ethanol	100mg/mL (186.4mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.8640mL	9.3200mL	18.6400mL
5mM	0.3728mL	1.8640mL	3.7280mL
10mM	0.1864mL	0.9320mL	1.8640mL
50mM	0.0373mL	0.1864mL	0.3728mL

生物活性

产品描述	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 9.8nM 和 2.6nM。
靶点/IC50	p300 HAT
靶点/IC50	0.06μM
体外研究	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 73nM.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.
体内研究	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.

推荐实验方法(仅供参考)

细胞实验:

Cell lines are plated in 96 well or 384 well plates and allowed to adhere for 24h. The cells are then treated with A-485 for 3, 4,or 5 days. Experiments are run in triplicate and the fraction of viable cells is determined using the Cell Viability Assay according to the manufacturer’s recommendations. For Thymidine incorporation assays, cells are treated with A-485 for 1,2, 3, or 4 days. Twenty four hours prior to the time point, tritiated thymidine is added and cells are incubated for an additional 24h. Genomic DNA is then isolated on filter plates.

动物实验:

The LuCap-77 CR prostate PDX model is used in this study. Donor tumors are dissociated and injected as a brie (1:2) into the right flank of 16 week old male C.B.-17 SCID mice on day 0 in a volume of 0.2mL. Tumors are size matched on day 26 postinoculation with a mean tumor volume of 211±3 (SEM) mm3 with dosing beginning on day 28. Mice are randomized into treatment groups using Studylog software based on tumor volume. LuCap-77 CR xenograft tumors are established in SCID mice and animals are dosed with A-485 as for 7 days. Three hours post the final dose, tumors are harvested and snap frozen on dry ice.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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