AP-1903 - CAS:195514-63-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	AP-1903
英文名称:	AP-1903
别名:	AP1903; Rimiducid;(S,2R,2'R)-(1R,1'R)-((((ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
CAS No:	195514-63-7	分子式:	C₇₈H₉₈N₄O₂₀	分子量:	1411.63
CAS No:	195514-63-7
分子式:	C₇₈H₉₈N₄O₂₀
分子量:	1411.63

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

A10971 AP-1903 ≥98% (psaitong)

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包装规格：

1mg 5mg 10mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO(超声)

产品描述：

基本信息

产品编号：A10971
产品名称：AP-1903
CAS:	195514-63-7	储存条件	粉末	-20℃	四年

分子式：	C78H98N4O20		溶于液体	-80℃	两年
分子量	1411.63
化学名：	[(1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[2-[[2-[3-[(1R)-3-(3,4-dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]ethylamino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
Solubility (25°C)	体外	DMSO	100mg/mL (70.84mM)
		Ethanol	100mg/mL (70.84mM)
		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	0.7084mL	3.5420mL	7.0840mL
5mM	0.1417mL	0.7084mL	1.4168mL
10mM	0.0708mL	0.3542mL	0.7084mL
50mM	0.0142mL	0.0708mL	0.1417mL

生物活性

产品描述	一种二聚化剂，其通过交联FKBP结构域起作用，启动Fas信号传导，引起凋亡。
靶点/IC₅₀	FKBP, in HT1080 cells EC50: 0.1nM	Fas receptor
体外研究	The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence,two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC50 of ≈0.1nM. Maximal killing occurred in the presence of 3 to 10nM Rimiducid (AP1903), and the IC50 is approximately 0.2nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment.
体内研究	Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg.

推荐实验方法(仅供参考)

细胞实验：
Cell Assay	Cloned HT1080 cell lines (ATCC CCL-121) retrovirally transduced with Fas constructs are prepared. Cell viability after overnight incubation with Rimiducid (0.01nM, 0.1nM, 1nM, 10nM, 100nM, 1000nM) is measured by Alamar Blue assay.For annexin V assays, sorted LV′VFas-transduced T cells (2×106 cells/mL) are incubated with 10 nM Rimiducid. Analyzed by flow cytometry.

动物实验:

Animal Administration

Mice

Male nu/nu mice are used. For injection, HTFasGH-3 cells are harvested from tissue culture dishes in PBS/0.1% glucose/10mM EDTA, washed, and resuspended in PBS/0.1% BSA/0.1% glucose at a concentration of 2×107 cells/mL. Between 2 and 4×106 cells are implanted into two i.m. sites. After 24h, mice are administered i.v. Rimiducid at 2mL/kg. After a further 24 h mice are killed and serum human GH concentrations are determined by ELISA.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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