Rucaparib - CAS:283173-50-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Rucaparib 促销
英文名称:	Rucaparib
别名:	鲁卡帕尼；瑞卡帕布；8-氟-2-(4-((甲胺基)甲基)苯基)-4,5-二氢-1H-氮杂卓并[5,4,3-cd]吲哚-6(3H)-酮 AG014699; PF-01367338；8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one
CAS No:	283173-50-2	分子式:	C₁₉H₁₈FN₃O	分子量:	323.36
CAS No:	283173-50-2
分子式:	C₁₉H₁₈FN₃O
分子量:	323.36
MDL:	MFCD11977252

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R10281 Rucaparib ≥98% (普西唐-psaitong)

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包装规格：

100mg in glass bottle

溶解性：

溶于DMSO（50mg/mL 超声）

产品描述：

基本信息

产品编号：R10281
产品名称：Rucaparib
CAS:	283173-50-2	储存条件	粉末	-20℃	四年

分子式：	C19H18FN3O		溶于液体	-80℃	两年
分子量	323.36			-20℃	一个月
化学名：	8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one
Solubility (25°C)	体外	DMSO	65mg/mL (201.01mM)
		Ethanol	32mg/mL (98.96mM)
		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	3.0925mL	15.4626mL	30.9253mL
5mM	0.6185mL	3.0925mL	6.1851mL
10mM	0.3093mL	1.5463mL	3.0925mL
50mM	0.0619mL	0.3093mL	0.6185mL

生物活性

产品描述	一种具有口服活性的、有效的 PARP 抑制剂，对 PARP1 的 Ki 值为 1.4nM，对其他八种 PARP 结构域也有亲和性。
靶点/IC₅₀	PARP1 (Cell-free assay) 1.4nM(Ki)
体外研究	Rucaparib is the most potent PARP inhibitor in enzyme assays (Ki, 1.4nM), and a possible N-demethylation metabolite of AG14644. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1μM in permeabilised D283Med cells.
体内研究	Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.

推荐实验方法(仅供参考)

激酶实验：
Kinase Assay	Inhibition of PARP activity in 5×103 D283Med cells is measured using various concentrations of Rucaparib (0-1μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica.

细胞实验:

Cell Assay

Medulloblastoma cell lines are seeded in 96-well plates at a density of 1×103, 3×103 and 3×103, respectively. At 24 hours(D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone.

动物实验:

Animal Administration

A single dose of temozolomide is administrated p.o. as a suspension in saline at 200mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078mg/kg free AG14644 only)], 1.0, and 10 mg/kg (for the mesylate salts equivalent to 0.79 and 7.9mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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