Niraparib

SKU: orb1304399

描述

Niraparib (MK-4827) is a potent and selective PARP1/2 inhibitor (IC50=3.8/2.1 nM) that impedes DNA repair, leading to apoptosis. It is widely used in oncology research, demonstrating antitumor efficacy in both cellular assays and in vivo models of BRCA-mutated and homologous recombination-deficient cancers.

研究领域

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号	1038915-60-4
MW	320.39
纯度	99.91% (May vary between batches)
分子式	C₁₉H₂₀N₄O
SMILES	C(N)(=O)C=1C=2C(=CN(N2)C3=CC=C(C=C3)[C@@H]4CCCNC4)C=CC1
靶点	Apoptosis,PARP
溶解性	DMSO:65.63 mg/mL (204.84 mM);Ethanol:60 mg/mL (187.27 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:6 mg/mL (18.73 mM)

生物活性

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靶点 IC50	PARP4:330 nM\|tankyrase 1:570 nM\|PARP2:2.1 nM\|PARP1:3.8 nM\|PARP3:1300 nM
体内	METHODS: To detect anti-tumor activity in vivo, Niraparib (25 mg/kg, administered orally four times per week) and PD-L1 (10 mg/kg, administered intraperitoneally twice per week) were administered to C57BL/6 mice bearing ovarian cancer tumor ID8 for eight weeks. RESULTS: Niraparib upregulated PD-L1 expression in ovarian tumors in vivo and synergized with PD-L1 blockade. METHODS: To detect anti-tumor activity in vivo, Niraparib (50 mg/kg, 0.5% methylcellulose) was administered by gavage to C57BL/6 mice bearing intracranial human-derived TNBC cell lines SUM149, MDA-MB-231Br, or MDA-MB-436 once daily for two weeks. RESULTS: In the BRCA mutant MDA-MB-436 model, Niraparib increased median survival and decreased tumor load. However, it did not increase in the BRCA mutant SUM149 or BRCA wild-type MDA-MB-231Br models, despite high concentrations in intracranial tumors.
体外	METHODS: The PDAC cell lines MIA-PaCa-2, PANC-1, Capan-1 and the OvCa cell lines OVCAR8, PEO1 were treated with Niraparib (0.1-200 µM) for 48 h, and the cells were assayed for viability using the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: The IC50 of Niraparib on MIA-PaCa-2, PANC-1, Capan-1, OVCAR8, and PEO1 cells were 26 µm, 50 µm, 15 µM, 20 µM, and 28 µM, respectively. . METHODS: Ovarian cancer cells SKOV3 and UWB1.289 were treated with Niraparib (0.5-15 µM) for 48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Niraparib upregulated the expression of PD-L1 in SKOV3 and UWB1.289 cells.
细胞研究	Proliferation assays were conducted in 96-well black viewplates, and 300 cells/well (250 cell/well for BRCA-1 wt) in culture medium, 190 μL/well (DMEM containing 10% FCS, 0.1 mg/mL penicillin-streptomycin, and 2 mM L-glutamine), were plated and incubated for 4 h at 37℃ under 5% CO2 atmosphere. Inhibitors were then added with serial dilutions, 10 μL/well to obtain the desired final compound concentration in 0.5% DMSO. The cells were then incubated for 7 days at 37℃ in 5% CO2 after which time viability was assessed. Briefly, with CellTiter-Blue solution prediluted 1:10 in medium, 100 μL/well was added and the cells left for 45 min at 37℃ under 5% CO2 and then a further 15 min at room temperature in the dark. The number of living cells was determined by reading the plate at fluorimeter, excitation at 550 nm and emission at 590 nm. Cell growth was expressed as the percentage growth with respect to vehicle treated cells. The concentration required to inhibit cell growth by 50% (CC50) was determined.(Only for Reference)

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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breast, damage, DNA, bioavailable, cancer, Apoptosis, anti-tumor, Inhibitor, MK-4827, MK4827, MK 4827, PARP2, PARP3, PARP1, PARP, ovarian, poly ADP ribose polymerase, Niraparib, orally, inhibit, lung, TANK-1, V-PARP

相似产品

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MSC778 [orb3173123]
CAS 号：
3098173-17-9
MW:
441.87
分子式：
C₂₂H₂₀ClN₃O₅
可选规格： 10 mg, 50 mg
Niraparib hydrochloride [orb1304290]
纯度：
99.90% (May vary between batches)
CAS 号：
1038915-64-8
MW:
356.85
分子式：
C₁₉H₂₁ClN₄O
可选规格： 2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 25 mg, 1 ml x 10 mM (in DMSO)
MK-4827 Racemate [orb1305758]
纯度：
99.86% (May vary between batches)
CAS 号：
1038915-75-1
MW:
320.39
分子式：
C₁₉H₂₀N₄O
可选规格： 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 mg, 1 ml x 10 mM (in DMSO)
Niraparib metabolite M1 HCl [orb2815838]
纯度：
99.20% (May vary between batches)
MW:
357.83
分子式：
C₁₉H₂₀ClN₃O₂
可选规格： 10 mg, 1 mg, 5 mg, 25 mg, 1 ml x 10 mM (in DMSO)
Niraparib metabolite M1 [orb1709021]
纯度：
99.65% (May vary between batches)
CAS 号：
1476777-06-6
MW:
321.37
分子式：
C₁₉H₁₉N₃O₂
可选规格： 25 mg, 5 mg, 10 mg, 1 mg, 1 ml x 10 mM (in DMSO)

质量保证

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化合物标识

PubChem CID

24958200 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	3098173-17-9
MW:	441.87
分子式：	C₂₂H₂₀ClN₃O₅

纯度：	99.90% (May vary between batches)
CAS 号：	1038915-64-8
MW:	356.85
分子式：	C₁₉H₂₁ClN₄O

纯度：	99.86% (May vary between batches)
CAS 号：	1038915-75-1
MW:	320.39
分子式：	C₁₉H₂₀N₄O

纯度：	99.20% (May vary between batches)
MW:	357.83
分子式：	C₁₉H₂₀ClN₃O₂

纯度：	99.65% (May vary between batches)
CAS 号：	1476777-06-6
MW:	321.37
分子式：	C₁₉H₁₉N₃O₂

Niraparib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

MSC778 [orb3173123]

Niraparib hydrochloride [orb1304290]

MK-4827 Racemate [orb1305758]

Niraparib metabolite M1 HCl [orb2815838]

Niraparib metabolite M1 [orb1709021]

质量保证

化合物标识

关键属性

实验方案信息

可选规格