瑞卡帕布磷酸盐|T6127|TargetMol

Rucaparib Phosphate
459868-92-9

￥258 1mg 起订

￥619 5mg 起订

￥987 10mg 起订

上海更新日期：2024-09-24

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产品详情:

中文名称：: 瑞卡帕布磷酸盐

英文名称：: Rucaparib Phosphate

CAS号：: 459868-92-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.1%

产品类别：: 抑制剂

货号：: T6127

Product Introduction

Bioactivity

名称	Rucaparib Phosphate
描述	Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.
细胞实验	Inhibition of PARP activity in 5000 exponentially growing D283Med cells was measured following treatment with a range of AG-014699 concentrations (0–1?μ), in comparison with DMSO-only controls. Maximally stimulated PARP activity was measured in replicate samples (n?3) of permeabilised cells by immunological detection of the amount of poly(ADP-ribose) (PAR) formed, using 10H anti-PAR antibody, during a 6-min incubation with NAD+ and oligonucleotide (substrate and activator) by reference to a PAR standard curve using a GCLP-validated assay described previously [2].
激酶实验	We measured inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation as described previously. The [32P]ADP-ribose incorporated into acid insoluble material was quantified using a PhosphorImager. Kis were calculated by nonlinear regression analysis [1].
动物实验	One or four daily doses of PARP inhibitor AG-014699 (1?mg/kg intraperitoneally (i.p.)) were given to CD-1 nude mice bearing established D283Med xenografts. At 0.5, 2, 6 and 24?h after the initial or fourth daily dose of AG-014699, three animals per time point were bled by cardiac puncture under general anaesthesia, and then killed. Plasma was separated from the blood samples using standard methods and stored at ?80°C. The brains and tumours were removed, snap frozen in liquid nitrogen and stored at ?80°C before analysis. Blood, tumour and brain tissue were removed from three untreated control animals and processed in the same way [2].
体外活性	AG14447（Rucaparib的磷酸盐）在酶测定中是高效的PARP抑制剂（Ki：1.4 nmol/L）[1]。在渗透的D283Med细胞中，Rucaparib (AG-014699) 以0.1, 0.4 和 1μ的浓度分别抑制了81.1%，96.8% 和97.1% 的PARP-1活性[2]。AG014699（≤10 μM）对带有突变BRCA1/2或XRCC3的细胞以及表观遗传学沉默BRCA1的UACC3199细胞具有细胞毒性，但对没有BRCA1/2或XRCC3突变或BRCA2突变为杂合子的细胞则无影响[3]。
体内活性	当以10mg/kg Rucaparib与temozolomide联合给药时，观察到治疗后第4至13天体重减轻，体重最低点范围从起始体重的83%至96%。以1mg/kg剂量，Rucaparib也显著增加了由temozolomide引起的体重减轻[1]。以1mg/kg、每日五次给药，AG-014699单独使用未引起任何明显毒性或对肿瘤生长产生影响，与仅用载体对照组比较。AG-014699与temozolomide的联合给药也导致所有小鼠的肿瘤完全消退，其中五分之三的小鼠实验期间肿瘤持续消退。MMR缺陷的D283Med异种移植物生长非常迅速，对单独使用temozolomide的响应极低（TGD仅为2天），在任何小鼠中未观察到肿瘤退缩[2]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 78 mg/mL (185.1 mM)
关键字	BRCA2 \| PARP \| BRCA1 \| inhibit \| Capan-1 \| PF 01367338 \| AG-014699 Phosphate \| Rucaparib Phosphate \| AG 014699 Phosphate \| MX-1 \| repair \| Rucaparib \| AG14644 \| AG014699 Phosphate \| SSB \| NF-κB \| H6PD \| PF01367338 Phosphate \| poly ADP ribose polymerase \| PF 01367338 Phosphate \| AG014699 \| AG 014699 \| Inhibitor \| PF-01367338 Phosphate \| PF01367338
相关产品	Niraparib \| Olaparib \| 3-Aminobenzamide \| Benzamide
相关库	抑制剂库 \| 已知活性化合物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

卡帕尼磷酸盐|||AG-014699 phosphate|||PF-01367338|||芦卡帕利|||AG-014699|||PF-01367338 phosphate|||瑞卡帕布磷酸盐|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子