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Fluzoparib/氟唑帕利 {[allProObj[0].p_purity_real_show]}

货号:A1474773 同义名: SHR3162; Fuzuloparib

Fluzoparib是一种口服有效的 PARP1 抑制剂,能够选择性地抑制 DNA 修复机制。它在癌症治疗中展现了优异的抗肿瘤活性。

Fluzoparib/氟唑帕利 化学结构 CAS号:1358715-18-0
Fluzoparib/氟唑帕利 化学结构
CAS号:1358715-18-0
Fluzoparib/氟唑帕利 3D分子结构
CAS号:1358715-18-0
Fluzoparib/氟唑帕利 化学结构 CAS号:1358715-18-0
Fluzoparib/氟唑帕利 3D分子结构 CAS号:1358715-18-0
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Fluzoparib/氟唑帕利 纯度/质量文件 产品仅供科研

货号:A1474773 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PARP PARP1 PARP2 PARP3 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

98%
AZD-2461 99%+
BGP-15 99%+
NU1025 +

PARP, IC50: 400 nM

98%
Benzamide +

PARP, IC50: 3.3 μM

98%
Picolinamide +

PARP, IC50: 95 μM

98%
AG14361 +++

PARP1, Ki: <5 nM

98+%
Iniparib 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

97%
UPF 1069 +

PARP1, IC50: 8.0 μM

++

PARP2, IC50: 0.3 μM

98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

+++

PARP2, Ki: 1.5 nM

99%+
Veliparib ++

PARP1, Ki: 5.2 nM

+++

PARP2, Ki: 2.9 nM

98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

99%+
Stenoparib ++++

PARP1, IC50: 1 nM

++++

PARP2, IC50: 1.2 nM

98%
Olaparib +++

PARP1, IC50: 5 nM

++++

PARP2, IC50: 1 nM

98%
Niraparib +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

98%
ME0328 +

PARP1, IC50: 6.3 μM

+

PARP3, IC50: 0.89 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Fluzoparib/氟唑帕利 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-231 2.5 µM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
GBC-SD 5 μM 4 hours Inhibited cell proliferation and enhanced radiosensitivity Cancer Manag Res. 2020 Nov 19;12:11833-11844
OVCA433 5 µM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
DOV13 625 nM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
BT-549 625 nM 3 h Inhibition of H2O2-induced PARylation Am J Cancer Res. 2019 Mar 1;9(3):608-618
HCCC-9810 10 μM 4 hours Inhibited cell proliferation and enhanced radiosensitivity Cancer Manag Res. 2020 Nov 19;12:11833-11844
MDA-MB-468-FR 80 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on drug-resistant MDA-MB-468-FR cells, results showed that the viability of drug-resistant cells was significantly higher than that of parental cells Front Oncol. 2022 Feb 18;12:819714
HCC1937-FR 60 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on drug-resistant HCC1937-FR cells, results showed that the viability of drug-resistant cells was significantly higher than that of parental cells Front Oncol. 2022 Feb 18;12:819714
MDA-MB-468 15 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on MDA-MB-468 cells, results showed that cell growth was significantly reduced with increasing Fluzoparib concentration Front Oncol. 2022 Feb 18;12:819714
HCC1937 6 mg/ml 48 hours Evaluate the cytotoxicity of Fluzoparib on HCC1937 cells, results showed that cell growth was significantly reduced with increasing Fluzoparib concentration Front Oncol. 2022 Feb 18;12:819714
NCI–H929B (H929B, bortezomib-resistant) 2.5, 5, 10 nM 24 hours To evaluate the effect of Fluzoparib on the viability and apoptosis of drug-resistant MM cells. Results showed that Fluzoparib significantly inhibited the proliferation of H929B cells and induced apoptosis. Biochem Biophys Rep. 2024 Jul 7;39:101781
NCI–H929 (H929) 2.5, 5, 10 nM 24 hours To evaluate the effect of Fluzoparib on the viability and apoptosis of MM cells. Results showed that Fluzoparib significantly inhibited the proliferation of H929 and H929B cells and induced apoptosis. Biochem Biophys Rep. 2024 Jul 7;39:101781

Fluzoparib/氟唑帕利 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice HCC1937-FR xenograft model Subcutaneous injection 25 mg/kg/bid (Fluzoparib), 5 mg/kg/bw (Chidamide) Twice daily for 21 days Evaluate the antitumor effects of Fluzoparib and Chidamide on HCC1937-FR xenograft model, results showed that the combination significantly inhibited tumor growth Front Oncol. 2022 Feb 18;12:819714
BALB/c nude mice Subcutaneous MM tumor model Oral 30 mg/kg Once daily for 13 days To evaluate the inhibitory effect of Fluzoparib on MM tumor growth in vivo. Results showed that Fluzoparib significantly suppressed tumor volumes and weights and promoted apoptosis of tumor tissue. Biochem Biophys Rep. 2024 Jul 7;39:101781

Fluzoparib/氟唑帕利 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL

Fluzoparib/氟唑帕利 技术信息

CAS号1358715-18-0
分子式C22H16F4N6O2
分子量 472.4
SMILES Code O=C1NN=C(CC2=CC=C(F)C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)C5=C1C=CC=C5
MDL No. MFCD32899277
别名 SHR3162; Fuzuloparib; HS10160
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 35 mg/mL(74.09 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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