Niraparib tosylate

別名: MK 4827 tosylate 中文名稱：尼拉帕尼甲苯磺酸鹽

目錄號(hào)：S7625 Purity: 99.99%

Niraparib tosylate是PARP1/PARP2的選擇性抑制劑，IC50分別為3.8 nM和2.1 nM。Niraparib可增加PARP-DNA復(fù)合體的形成，并導(dǎo)致DNA損傷、凋亡和細(xì)胞死亡。

Niraparib tosylate Chemical Structure

CAS: 1038915-73-9

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1449.63	現(xiàn)貨
5mg	959.15	現(xiàn)貨
25mg	3251.76	現(xiàn)貨
100mg	8165.6	現(xiàn)貨
1g	12039.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Niraparib tosylate相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 凋亡分子化合物庫(kù) DNA損傷/ DNA修復(fù)化合物庫(kù) 細(xì)胞周期化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
MDA-MB-436	Antitumor assay	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
MDA-MB-436	Antitumor assay	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
MDA-MB-436	Antitumor assay	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
MDA-MB-436	Antitumor assay	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
MDA-MB-436	Antitumor assay	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
MDA-MB-436	Antitumor assay	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
HeLa	Antiproliferative assay		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
Capan1	Antiproliferative assay		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
HeLa	Antiproliferative assay		7 days	Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay, CC50 = 0.033 μM.	19873981
MDA-MB-436	Antiproliferative 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 = 0.018 μM.	19873981
Jurkat	Function assay		96 hrs	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
Jurkat	Function assay		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
A549	Cytotoxicity assay		5 to 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
SUM1315MO2	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
DoTc2-4510	Cytotoxicity assay		5 to 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
SUM149PT	Cytotoxicity assay		5 to 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
HeLa	Cytotoxicity assay		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
UWB1.289	Cytotoxicity assay		5 to 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
HeLa	Cytotoxicity assay		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
UWB1.289	Cytotoxicity assay		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
A549	Cytotoxicity assay		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
BT20	Cytotoxicity assay		5 to 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
HeLa	Function assay			Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC90 = 0.045 μM.	19873981
HeLa	Function assay			Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC50 = 0.004 μM.	19873981
CAPAN-1	Function assay			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
HeLa	Function assay			Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, EC50 = 0.004 μM.	25761096
A2780	Function assay			Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC50 = 0.004 μM.	25761096
MDA-MB-436	Cytotoxicity assay			Cytotoxicity against human MDA-MB-436 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation, CC50 = 0.018 μM.	25761096
HeLa	Function assay			Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.046 μM.	25761096
CAPAN-1	Function assay			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
A2780	Function assay			Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.052 μM.	25761096
Capan1	Cytotoxicity assay			Cytotoxicity against BRCA2-deficient human Capan1 cells, CC50 = 0.09 μM.	25761096
Capan1	Cytotoxicity assay			Cytotoxicity against BRCA2-deficient human Capan1 cells, EC50 = 0.65 μM.	26652717
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

PARP2 ^[3] (Cell-free assay)	PARP1 ^[3] (Cell-free assay)
2.1 nM	3.8 nM

體外研究(In Vitro)
體外研究活性	微摩爾級(jí)濃度的niraparib使來(lái)自于肺癌、乳腺癌以及前列腺癌的腫瘤細(xì)胞對(duì)放射線敏感（不依賴于它們的p53狀態(tài)），而對(duì)來(lái)自于正常組織的細(xì)胞沒(méi)有此作用。Niraparib同樣還可以使腫瘤細(xì)胞對(duì)過(guò)氧化氫敏感、在DNA復(fù)制時(shí)，將過(guò)氧化氫誘導(dǎo)的單鏈斷裂轉(zhuǎn)變?yōu)殡p鏈斷裂^[5]。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	V-C8細(xì)胞
	濃度	50 nM
	孵育時(shí)間	24 h
	方法	用PARP抑制劑MK-4827對(duì)中國(guó)倉(cāng)鼠細(xì)胞V-C8（BRCA2-negative）進(jìn)行處理，24小時(shí)后，洗滌并將細(xì)胞孵育在不含此化合物的培養(yǎng)基中5-7天，直到形成克隆。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)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可以增強(qiáng)放射線對(duì)多種人類(lèi)腫瘤異種移植的作用，無(wú)論是在p53野生型或是p53突變體。MK-4827在給藥后1小時(shí)降低腫瘤中PAR水平并持續(xù)效果24小時(shí)^[1]。MK-4827體內(nèi)給藥能延長(zhǎng)放射線處理后的動(dòng)物壽命。MK-4827和放射治療結(jié)合，顯著提高腫瘤中裂解的caspase-3和γ-H2AX的水平^[4]。
動(dòng)物實(shí)驗(yàn)	Animal Models	雌性裸鼠(Ncr Nu/Nu)
	Dosages	25或50 mg/kg
	Administration	口服

參考文獻(xiàn)
[1] Wang L, et al. Invest New Drugs. 2012, 30(6):2113-20. [2] Patel AG, et al. J Biol Chem. 2012, 287(6):4198-210. [3] Jones P, et al. J Med Chem. 2009, 52(22):7170-85. [4] Mueller S, et al. Anticancer Res. 2013, 33(3):755-62. [5] Bridges KA, et al. oncotarget. 2014, 5(13):5076-86. + 展開(kāi)

參考文獻(xiàn)

[1] Wang L, et al. Invest New Drugs. 2012, 30(6):2113-20.
[2] Patel AG, et al. J Biol Chem. 2012, 287(6):4198-210.
[3] Jones P, et al. J Med Chem. 2009, 52(22):7170-85.

[4] Mueller S, et al. Anticancer Res. 2013, 33(3):755-62.
[5] Bridges KA, et al. oncotarget. 2014, 5(13):5076-86.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	492.59	分子式	C₁₉H₂₀N₄O.C₇H₈O₃S
CAS號(hào)	1038915-73-9	SDF	Download Niraparib tosylate SDF
Smiles	CC1=CC=C(C=C1)S(=O)(=O)O.C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 99 mg/mL ( (200.97 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 99 mg/mL ( (200.97 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 98 mg/mL ( (198.94 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 98 mg/mL ( (198.94 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 99 mg/mL ( (200.97 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Niraparib tosylate

產(chǎn)品質(zhì)控

Niraparib tosylate相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持