2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Rucaparib

Rucaparib  (Synonyms: 瑞卡帕布; AG014699; PF-01367338)

目录号: HY-10617A 纯度: 99.97%
COA 产品使用指南

摩尔计算器

Rucaparib (AG014699) 是一种口服有效的 PARP 蛋白 (PARP-1, PARP-2 and PARP-3) 抑制剂，对 PARP-1 的 Ki 为 1.4 nM。Rucaparib 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。

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Rucaparib Chemical Structure

Rucaparib Chemical Structure

CAS No. : 283173-50-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥825
In-stock
5 mg ￥750
In-stock
10 mg ￥1300
In-stock
50 mg ￥3500
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Rucaparib:

Rucaparib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 38 篇科研文献

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

IC50 & Target[1][2]

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
32.21 μM
Compound: 2; AG014699
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
DLD-1 IC50
0.027 μM
Compound: 2
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
[PMID: 34570508]
GBM EC50
> 100000 nM
Compound: Rucaparib
Cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst staining based assay
Cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst staining based assay
[PMID: 32527552]
GBM EC50
> 100000 nM
Compound: Rucaparib
Synergistic cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs in presence of temozolomide by Hoechst staining based assay
Synergistic cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs in presence of temozolomide by Hoechst staining based assay
[PMID: 32527552]
GBM IC50
2262 nM
Compound: Rucaparib
Synergistic antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs in presence of temozolomide by Edu incorporation assay
Synergistic antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs in presence of temozolomide by Edu incorporation assay
[PMID: 32527552]
GBM IC50
53443 nM
Compound: Rucaparib
Antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs by Edu incorporation assay
Antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs by Edu incorporation assay
[PMID: 32527552]
HT-22 IC50
57 μM
Compound: 53
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 36876904]
LoVo GI50
144 nM
Compound: 4; AG014699
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
[PMID: 26652717]
LoVo EC50
4.69 nM
Compound: 4; AG014699
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
[PMID: 26652717]
MCF7 CC50
19.47 μM
Compound: AG014699
Anticancer activity against human MCF7 cells after 96 hrs by MTT assay
Anticancer activity against human MCF7 cells after 96 hrs by MTT assay
[PMID: 26342868]
MCF7 IC50
6.61 μM
Compound: 2; AG014699
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
MDA-MB-231 IC50
39 μM
Compound: Ruc; Rib
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 35707158]
MDA-MB-436 CC50
3 μM
Compound: AG014699
Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay
Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay
[PMID: 26342868]
MX1 IC50
6.51 μM
Compound: 2; AG014699
Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 34656898]
OVCAR-3 IC50
3.31 μM
Compound: Rucaparib
Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay
Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay
[PMID: 29456106]
U-87MG ATCC IC50
20 μM
Compound: Ruc; Rib
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 35707158]
体外研究
(In Vitro)

Rucaparib（0.1-100 μM；24 小时）具有细胞毒性，在 Capan-1（BRCA2 突变体）细胞中的 LC50 为 5 μM，在 MX-1（BRCA1 突变体）细胞中仅为 100 nM[2]。
Rucaparib 的放射增敏作用是由于其下游抑制了 NF-κB 的激活，并且这种作用与单链断裂 (SSB) 修复抑制无关。Rucaparib 可以靶向由 DNA 损伤激活的 NF-κB，并克服传统 NF-κB 抑制剂所产生的毒性，同时不会损害其他重要的炎症功能[5]。
在透化的 D283Med 细胞中，Rucaparib 在浓度为 1 μM 时， 对 PARP-1 活性的抑制率达到了 97.1%[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rucaparib 相关抗体:
体内研究
(In Vivo)

Rucaparib (AG014699) 和 AG14584 显著增加 Temozolomide 的毒性。Rucaparib (1 mg/kg) 显著增加 Temozolomide (HY-17364) 引起的体重减轻。Rucaparib (0.1 mg/kg) 使 Temozolomide 引起的肿瘤生长延迟增加 50%[1]。
Rucaparib（i.p.; 10 mg/kg 或 p.o. ; 50-150 mg/kg；每天服用，每周 5 天，持续 6 周）显著抑制肿瘤生长，并出现一例肿瘤完全消退和两例持续的部分消退[2]。
Rucaparib（150 mg/kg; 口服; 每周一次，共持续 6 周，或每周三次，共持续 6 周）具有最强的抗肿瘤作用，出现了 3 例肿瘤完全消退[2]。
Rucaparib 增强了 Temozolomide 的抗肿瘤活性，并在 NB1691 和 SHSY5Y 异种移植瘤中显示出完全且持续的肿瘤消退[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells[2]
Dosage: 10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
Administration: IP or PO
Result: Significantly inhibited the growth of the tumor.
Clinical Trial
分子量

323.36

Formula

C19H18FN3O
CAS 号
性状

固体

颜色

Off-white to yellow

中文名称

瑞卡帕布；鲁卡帕尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (77.31 mM; ultrasonic and adjust pH to 4 with HCl; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0925 mL 15.4626 mL 30.9253 mL
5 mM 0.6185 mL 3.0925 mL 6.1851 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.73 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.73 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.97%

COA (193 KB) HNMR (257 KB) RP-HPLC (242 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献

Rucaparib 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0925 mL 15.4626 mL 30.9253 mL 77.3132 mL
5 mM 0.6185 mL 3.0925 mL 6.1851 mL 15.4626 mL
10 mM 0.3093 mL 1.5463 mL 3.0925 mL 7.7313 mL
15 mM 0.2062 mL 1.0308 mL 2.0617 mL 5.1542 mL
20 mM 0.1546 mL 0.7731 mL 1.5463 mL 3.8657 mL
25 mM 0.1237 mL 0.6185 mL 1.2370 mL 3.0925 mL
30 mM 0.1031 mL 0.5154 mL 1.0308 mL 2.5771 mL
40 mM 0.0773 mL 0.3866 mL 0.7731 mL 1.9328 mL
50 mM 0.0619 mL 0.3093 mL 0.6185 mL 1.5463 mL
60 mM 0.0515 mL 0.2577 mL 0.5154 mL 1.2886 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rucaparib283173-50-2AG014699 PF-01367338瑞卡帕布鲁卡帕尼AG 014699AG-014699PF01367338PF 01367338PF-01367338PARPpoly ADP ribose polymeraseAG14644Capan-1BRCA2MX-1BRCA1NF-κBSSBrepairH6PDInhibitorinhibitorinhibit

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