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Niraparib (MK-4827)

中文名稱：尼拉帕尼

Niraparib (MK4827)是一種口服有效的選擇性PARP-1和PARP-2抑制劑，可在有BRCA和PTEN功能缺陷的臨床腫瘤模型中引起合成致死性。Niraparib 可形成PARP–DNA復(fù)合物并導(dǎo)致DNA損傷、凋亡和細(xì)胞死亡。Phase 3。

Niraparib (MK-4827) Chemical Structure

Niraparib (MK-4827) Chemical Structure

CAS: 1038915-60-4

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1392.3 現(xiàn)貨
5mg 647.22 現(xiàn)貨
50mg 1941.16 現(xiàn)貨
200mg 4668.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Niraparib (MK-4827)相關(guān)產(chǎn)品

相關(guān)信號通路圖

PARP Signaling Pathways

PARP信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
Antitumor assay MDA-MB-436 50 mg/kg 33 days Antitumor activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant xenografted in CD1 mouse assessed as tumor regression at 50 mg/kg, po bid for 33 days 19873981
Antitumor assay MDA-MB-436 100 mg/kg 33 days Antitumor activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant xenografted in CD1 mouse assessed as tumor regression at 100 mg/kg, po qd for 33 days 19873981
Antitumor assay MDA-MB-436 80 mg/kg 1 to 2 weeks Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor growth inhibition at 80 mg/kg, po qd for 1 to 2 weeks 25761096
Antitumor assay MDA-MB-436 80 mg/kg 4 weeks Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as complete and sustained tumor regression at 80 mg/kg, po qd for 4 weeks 25761096
Antitumor assay MDA-MB-436 80 mg/kg 3 weeks Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor shrinkage at 80 mg/kg, po qd for 3 weeks 25761096
Antitumor assay MDA-MB-436 50 mg/kg Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor growth inhibition at 50 mg/kg, po administered daily 25761096
UWB1.289 cells Cytotoxicity assay 5-7 days Cytotoxicity against human UWB1.289 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50=0.056 μM 25761096
SUM149PT cells Cytotoxicity assay 5-7 days Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50=0.024 μM 25761096
DoTc2-4510 cells Cytotoxicity assay 5-7 days Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50=0.023 μM 25761096
SUM1315MO2 cells Cytotoxicity assay 12 days Cytotoxicity against human SUM1315MO2 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 12 days by CellTiter-Blue assay, CC50=0.02 μM 25761096
MDA-MB-436 cells Proliferation assay 6 days Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay, CC50=18 nM 19873981
A549 cells Cytotoxicity assay 5-7 days Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50=0.011 μM 25761096
BT20 cells Cytotoxicity assay 5-7 days Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50=2.2 μM 25761096
Antiproliferative assay HeLa 7 days Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay, CC50 = 0.033 μM. 19873981
Antiproliferative assay Capan1 13 days Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay, CC50 = 0.09 μM. 19873981
Antiproliferative assay HeLa 7 days Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay, CC50 = 0.86 μM. 19873981
Function assay Jurkat 96 hrs Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay, EC50 = 31 μM. 23850199
Cytotoxicity assay HeLa 5 to 7 days Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.034 μM. 25761096
Cytotoxicity assay HeLa 5 to 7 days Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.852 μM. 25761096
Cytotoxicity assay UWB1.289 5 to 7 days Cytotoxicity against human UWB1.289 cells expressing BRCA1 assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.975 μM. 25761096
Cytotoxicity assay A549 5 to 7 days Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 1.76 μM. 25761096
Capan1 cells Cytotoxicity assay Cytotoxicity against BRCA2-deficient human Capan1 cells, CC50=0.09 μM 25761096
HeLa cells Function assay Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC50=0.004 μM 19873981
Jurkat cells Function assay Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide, EC50=0.2 μM 23850199
Function assay HeLa Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC90 = 0.045 μM. 19873981
Function assay CAPAN-1 Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC50 = 0.0035 μM. 25761096
Function assay HeLa Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, EC50 = 0.004 μM. 25761096
Function assay A2780 Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC50 = 0.004 μM. 25761096
Cytotoxicity assay MDA-MB-436 Cytotoxicity against human MDA-MB-436 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation, CC50 = 0.018 μM. 25761096
Function assay HeLa Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.046 μM. 25761096
Function assay CAPAN-1 Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.05 μM. 25761096
Function assay A2780 Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.052 μM. 25761096
Cytotoxicity assay Capan1 Cytotoxicity against BRCA2-deficient human Capan1 cells, EC50 = 0.65 μM. 26652717
qHTS assay TC32 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
qHTS assay A673 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
qHTS assay NB1643 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
qHTS assay A673 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
qHTS assay BT-37 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
qHTS assay SK-N-MC qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
qHTS assay NB-EBc1 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
qHTS assay LAN-5 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
qHTS assay SK-N-MC qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
qHTS assay TC32 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
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生物活性

產(chǎn)品描述 Niraparib (MK4827)是一種口服有效的選擇性PARP-1和PARP-2抑制劑，可在有BRCA和PTEN功能缺陷的臨床腫瘤模型中引起合成致死性。Niraparib 可形成PARP–DNA復(fù)合物并導(dǎo)致DNA損傷、凋亡和細(xì)胞死亡。Phase 3。
靶點(diǎn)
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
2.1 nM 3.8 nM
體外研究(In Vitro)
體外研究活性 在完整細(xì)胞試驗中，MK-4827抑制PARP的活性，EC50為4 nM，并抑制攜帶BRCA-1和BRCA-2突變的癌細(xì)胞的增殖，IC50為10-100 nM。它能有效地抑制PARP-1和PARP-2，IC分別為3.8 nM和2.1 nM。它對PARP-3, V-PARP和tankyrase-1的選擇性低100倍以上，IC50分別為1300、330、570 nM。MK-4827能夠抑制攜帶有天然BRCA-1和BRCA-2突變的癌細(xì)胞的增殖、通過RNA干擾抑制BRCA-1缺陷的Hela細(xì)胞的生長。在攜帶BRCA-1突變的MDA-MB-436人類乳腺腺癌的細(xì)胞中，MK-4827的CC50=18 nM；而在BRCA-2缺陷的CAPAN-1人胰腺癌細(xì)胞中，CC50=90 nM。而正常人類前列腺和乳腺上皮細(xì)胞對MK-4827具有耐藥性，在微摩爾范圍內(nèi)具有抗凋亡作用，說明這些PARP抑制劑在具有BRCA-1和BRCA-2突變的癌細(xì)胞中具有選擇性細(xì)胞毒性，對周圍組織影響小[2]。
細(xì)胞實驗 細(xì)胞系 BRCA1基因沉默的Hela細(xì)胞
濃度 系列稀釋濃度
孵育時間 7天
方法 將細(xì)胞置于96孔黑色viewplates中，細(xì)胞密度為300/孔，每孔含190 μLDMEM培養(yǎng)基(含10%胎牛血清，0.1 mg/mL青-鏈霉素雙抗，2 mM L-谷氨酰胺)，在37℃、5% CO2的細(xì)胞培養(yǎng)箱中培養(yǎng)4小時。將系列稀釋的抑制劑加入其中，每孔10 μL，使化合物濃度達(dá)到工作濃度、DMSO為0.5%。然后在細(xì)胞在細(xì)胞培養(yǎng)箱中培養(yǎng)7天。7天后，測定細(xì)胞活力。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot c-PARP /c-caspase 3 / γ-H2AX 29158830
Immunofluorescence Rad51 / Geminin 27614696
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 MK-4827能夠顯著增強(qiáng)輻射對人類腫瘤移植體（p53野生型或p53突變型）的效果[1]。在體內(nèi)實驗中，其耐受良好。單獨(dú)使用時，在BRCA-1缺陷型移植瘤模型中具有一定功效[2]。
動物實驗 Animal Models 雌性裸鼠
Dosages 25 mg/kg每日兩次或50 mg/kg每日一次
Administration 口服
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05289648 Not yet recruiting
Endometrial Cancer|Serous Adenocarcinoma|Uterine Neoplasm
Sir Mortimer B. Davis - Jewish General Hospital
 May 1 2024 Early Phase 1
NCT06077877 Recruiting
Neoplasms
GlaxoSmithKline
 October 24 2023 Phase 1|Phase 2
NCT05666349 Withdrawn
Recurrent Glioblastoma
University College London|GlaxoSmithKline
 October 13 2023 Phase 1

化學(xué)信息&溶解度

分子量 320.39 分子式

C19H20N4O
CAS號 1038915-60-4 SDF Download Niraparib (MK-4827) SDF
Smiles C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 64 mg/mL ( (199.75 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 64 mg/mL (199.75 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
How to reconstitute the compound for in vivo studies?

回答：
You can use the formulation 1% CMC-Na (suspension) for oral administration.

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