Veliparib (ABT-888)

別名: NSC 737664 中文名稱：維利帕尼

目錄號：S1004 Purity: 99.94%

Veliparib (ABT-888, NSC 737664)是一種有效的PARP1和PARP2抑制劑，無細胞試驗中K_i分別為5.2 nM和2.9 nM，對SIRT2沒有活性。Veliparib 可增加自噬和凋亡。Phase 3。

Veliparib (ABT-888) Chemical Structure

CAS: 912444-00-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1277.12	現(xiàn)貨
10mg	973.01	現(xiàn)貨
50mg	3010.72	現(xiàn)貨
200mg	6470.1	現(xiàn)貨
1g	10401.3	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.94%

99.94

Veliparib (ABT-888)相關(guān)產(chǎn)品

相關(guān)靶點	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	點擊展開
相關(guān)產(chǎn)品	XAV-939 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	點擊展開
相關(guān)化合物庫	FDA藥物庫天然產(chǎn)物庫凋亡分子化合物庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
PC-3	Growth Inhibition Assay	10 μM		Induces a significant inhibition in colony formation?	21571912
C41	Function assay			Inhibition of PARP1 in human C41 cells, EC50 = 0.002 μM.	19143569
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
ML-2	Growth Inhibition Assay			IC50=49.7856 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=47.3791 μM	SANGER
KYSE-150	Growth Inhibition Assay			IC50=18.9986 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=18.5119 μM	SANGER
H9	Growth Inhibition Assay			IC50=18.2833 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=17.6294 μM	SANGER
GP5d	Growth Inhibition Assay			IC50=17.053 μM	SANGER
DEL	Growth Inhibition Assay			IC50=16.6717 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=16.5325 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=16.2042 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=15.9589 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=14.5565 μM	SANGER
DU-145	Growth Inhibition Assay			IC50=13.9053 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=13.5389 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=13.166 μM	SANGER
HEC-1	Growth Inhibition Assay			IC50=12.9196 μM	SANGER
KY821	Growth Inhibition Assay			IC50=12.485 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=12.4752 μM	SANGER
DT40	Cytotoxic Assay		72 h	Cytotoxicity against chicken BRCA2-deficient DT40 cells	24922587
Daoy	Growth Inhibition Assay			IC50=19.5649 μM	SANGER
T98G	Growth Inhibition Assay			IC50=44.8517 μM	SANGER
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LoVo	Cytotoxicity assay	0.4 uM	5 days	Potentiation of -induced cytotoxicity in human LoVo cells assessed as GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 6.203 μM.	26652717
VC8	Cytotoxicity assay		3 days	Cytotoxicity against Chinese hamster VC8 cells harboring BRCA2 deficient after 3 days by CCK8 assay, CC50 = 2.344 μM.	29335205
LoVo	Function assay		30 mins	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM.	26652717
HCT-116	Kinase Assay	0.5 μM	24 h	PARP activity decreases	23054213
UM-SCC1	Cytotoxic Assay	10 μM	24 h	Reduces the cell viability	21912620
FaDu	Cytotoxic Assay	10 μM	24 h	Reduces the cell viability	21912620
LoVo	Function assay		30 mins	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM.	26652717
MHH-PREB-1	Growth Inhibition Assay			IC50=45.7585 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=45.6389 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=7.79704 μM	SANGER
SK-MEL-24	Growth Inhibition Assay			IC50=7.81924 μM	SANGER
COLO-680	Growth Inhibition Assay			IC50=6.21406 μM	SANGER
Jurkat	Kinase Assay		96 h	Inhibition of PARP1 assessed as reduction of cell viability with EC50 of 3 μM	23850199
Capan1	Growth Inhibition Assay		72 h	Antiproliferative activity against BRCA2 gene mutated human Capan1 cells with IC50 of 39.7 μM	24398383
ML-1	Apoptotic Assay	2.5 μM	24 h	Synergistically enhances TRAIL-induced apoptosis in ML-1 cells	24895135
HCC1806	Growth Inhibition Assay			IC50=5.75173 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=8.43603 μM	SANGER
C41	Kinase Assay		30 min	Inhibition of PARP1 with EC50 of 0.002 μM	19888760
MOLT-13	Growth Inhibition Assay			IC50=29.3814 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=29.3814 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=29.3748 μM	SANGER
697	Growth Inhibition Assay			IC50=29.0235 μM	SANGER
LB771	Growth Inhibition Assay			IC50=28.8373 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=12.4663 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=10.434 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=9.8862 μM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=8.89266 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=30.4241 μM	SANGER
L-363	Growth Inhibition Assay			IC50=29.4798 μM	SANGER
KU812	Growth Inhibition Assay			IC50=32.3642 μM	SANGER
A2780	Growth Inhibition Assay			IC50=30.7457 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=33.6001 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=33.3889 μM	SANGER
NB14	Growth Inhibition Assay			IC50=40.7031 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=5.45409 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=3.12841 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=1.0798 μM	SANGER
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
NCI-H510A	Growth Inhibition Assay			IC50=47.9034 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=20.7455 μM	SANGER
A388	Growth Inhibition Assay			IC50=21.9091 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=23.1363 μM	SANGER
HCC1937	Growth Inhibition Assay			IC50=24.746 μM	SANGER
TGBC11TKB	Growth Inhibition Assay			IC50=25.6863 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=25.8969 μM	SANGER
NCI-H2029	Growth Inhibition Assay			IC50=26.4238 μM	SANGER
HLE	Growth Inhibition Assay			IC50=27.054 μM	SANGER
NCI-H1693	Growth Inhibition Assay			IC50=27.2898 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=27.7246 μM	SANGER
BEN	Growth Inhibition Assay			IC50=27.9566 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=36.952 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=41.3063 μM	SANGER
MDA-MB-361	Growth Inhibition Assay			IC50=43.8414 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=43.9532 μM	SANGER
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
LoVo	Function assay		30 mins	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00594 μM.	26652717
EM-2	Growth Inhibition Assay			IC50=29.4901 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=33.3599 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=35.5868 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=35.8499 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=36.7345 μM	SANGER
H4	Growth Inhibition Assay			IC50=37.567 μM	SANGER
T47D	Growth Inhibition Assay			IC50=37.7018 μM	SANGER
CAL-54	Growth Inhibition Assay			IC50=37.966 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=39.3304 μM	SANGER
SW982	Growth Inhibition Assay			IC50=38.0998 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=41.2771 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=41.4818 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=42.2538 μM	SANGER
JVM-2	Growth Inhibition Assay			IC50=42.9207 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=43.5691 μM	SANGER
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

ABT-888增強常見癌癥療法的效果，比如放射療法和烷基化劑。

靶點

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
2.9 nM(Ki)	5.2 nM(Ki)

體外研究(In Vitro)
體外研究活性	ABT-888有效抑制PARP，作用于PARP-1和PARP-2時K_i值分別為5.2和2.9 nM。ABT-888降低肺癌H460細胞中克隆基因的存活率，且抑制DNA修復。^[1] ABT-888抑制C41細胞，EC50為2 nM。^[2] ABT-888和放射物聯(lián)用減少腫瘤血管的形成。^[3]
激酶實驗	體外PARP實驗
激酶實驗	在含有50 mM Tris (pH 為8.0), 1 mM DTT,和 4 mM MgCl₂的緩沖溶液中進行酶活性測定。PARP反應(yīng)包含1.5 μM [³H]-NAD⁺ (1.6 μCi/mmol), 200 nM 生物素組蛋白 H1, 200 nM slDNA,及1 nM PARP-1或4 nM PARP-2酶。在加有100 μL 反應(yīng)液的 96孔板上進行SPA檢測。在50 μL含有PARP和DNA的2×酶液混合物中加入50 μL 2×NAD⁺基底混合物，反應(yīng)開始。加入150 μL 1.5 mM 苯甲酰胺反應(yīng)停止。170uL反應(yīng)終止液轉(zhuǎn)移到鏈霉親和素包被的閃熔鍍層上，溫育1小時，用微型板塊閃爍計數(shù)器計數(shù)。
細胞實驗	細胞系	C41細胞
	濃度	10 μM 左右
	孵育時間	0.5小時
	方法	在96孔板上用ABT-888處理C41細胞0.5小時。用1 mM H₂O₂破壞DNA10分鐘，PARP被激活。用冰凍的PBS沖洗細胞，然后用預冷的甲醇/丙酮（按7:3比例混合）在−20^oC下固定10 分鐘。風干后，用PBS再溶解，然后用溶有5%脫脂奶粉的PBS- Tween封閉液(0.05%)在室溫下阻斷0.5小時。細胞和PAR抗體按1：50比例在封閉液中室溫下溫育1小時，然后用PBS-Tween-20沖洗5分鐘，然后加入熒光素-5(6)-異硫氰酸酯 (FITC)-聯(lián)用的二抗和1μg/mL DAPI封閉液中室溫下溫育1小時。PBS-Tween-20沖洗5分鐘后，用熒光微型版計數(shù)器分析數(shù)據(jù)。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38		22678161
	Immunofluorescence	HuR BRCA1		28687616
	Growth inhibition assay	Cell viability (TNBC cell lines) Cell viability (melanoma cells)		27880910

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	ABT-888推遲NCI-H460 移植瘤模型的腫瘤生長。ABT-888在B16F10 和9L 移植瘤模型中抑制PARP，從而增強temozolomide的抗癌活性。^[1] ABT-888和其他細胞毒素藥劑聯(lián)用作用于MX-1移植瘤模型時顯示出強抗癌效力。^[2] 在A375和 Colo829移植瘤模型中按腫瘤大小，每千克分別加3和12.5 mg ABT-888，可以看到腫瘤內(nèi)95%以上PAR被抑制。^[4]
動物實驗	Animal Models	攜帶NCI-H460, H460, B16F10和9L移植瘤的C57BL/6鼠
	Dosages	25或3.125 mg/kg
	Administration	口服處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT03044795	Withdrawn	Cancer	University Medical Center Groningen\|AbbVie\|Dutch Cancer Society	November 2019	Phase 2
NCT02723864	Completed	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	August 9 2017	Phase 1
NCT02483104	Completed	Ovarian Cancer	AbbVie	July 2015	Phase 1

參考文獻
[1] Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737. [2] Penning TD, et al, J Med Chem, 2009, 52(2), 514-523. [3] Albert JM, et al, Clin Cancer Res, 2007, 13(10), 3033-3042. [4] Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885. + 展開

參考文獻

[1] Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737.
[2] Penning TD, et al, J Med Chem, 2009, 52(2), 514-523.
[3] Albert JM, et al, Clin Cancer Res, 2007, 13(10), 3033-3042.

[4] Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.

+ 展開

化學信息&溶解度

分子量	244.29	分子式	C₁₃H₁₆N₄O
CAS號	912444-00-9	SDF	Download Veliparib (ABT-888) SDF
Smiles	CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 49 mg/mL ( (200.58 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 48 mg/mL ( (196.48 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 49 mg/mL ( (200.58 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 49 mg/mL ( (200.58 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : 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
=	×	×

稀釋計算器分子量計算器

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）

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

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

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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Veliparib (ABT-888)

產(chǎn)品質(zhì)控

Veliparib (ABT-888)相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

技術(shù)支持