Veliparib (ABT-888)

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.

CAS No. 912444-00-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
200mg	JPY 118500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（226）

製品安全説明書

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Veliparib (ABT-888)関連製品

関連ターゲット	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

PARPシグナル伝達経路

PARP阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
LoVo	Cytotoxicity assay	0.4 uM	5 days	Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 6.203 μM.	26652717
FaDu	Cytotoxic Assay	10 μM	24 h	Reduces the cell viability	21912620
UM-SCC1	Cytotoxic Assay	10 μM	24 h	Reduces the cell viability	21912620
HCT-116	Kinase Assay	0.5 μM	24 h	PARP activity decreases	23054213
ML-1	Apoptotic Assay	2.5 μM	24 h	Synergistically enhances TRAIL-induced apoptosis in ML-1 cells	24895135
PC-3	Growth Inhibition Assay	10 μM		Induces a significant inhibition in colony formation	21571912
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
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
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
DT40	Cytotoxic Assay		72 h	Cytotoxicity against chicken BRCA2-deficient DT40 cells	24922587
Capan1	Growth Inhibition Assay		72 h	Antiproliferative activity against BRCA2 gene mutated human Capan1 cells with IC50 of 39.7 μM	24398383
Jurkat	Kinase Assay		96 h	Inhibition of PARP1 assessed as reduction of cell viability with EC50 of 3 μM	23850199
C41	Kinase Assay		30 min	Inhibition of PARP1 with EC50 of 0.002 μM	19888760
SK-MEL-24	Growth Inhibition Assay			IC50=7.81924 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=7.79704 μM	SANGER
COLO-680	Growth Inhibition Assay			IC50=6.21406 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=5.75173 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
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
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 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
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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
C41	Function assay			Inhibition of PARP1 in human C41 cells, EC50 = 0.002 μM.	19143569
NCI-H720	Growth Inhibition Assay			IC50=8.43603 μM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=8.89266 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=9.8862 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=10.434 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=12.4663 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=12.4752 μM	SANGER
KY821	Growth Inhibition Assay			IC50=12.485 μM	SANGER
HEC-1	Growth Inhibition Assay			IC50=12.9196 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=13.166 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=13.5389 μM	SANGER
DU-145	Growth Inhibition Assay			IC50=13.9053 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=14.5565 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=15.9589 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=16.2042 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=16.5325 μM	SANGER
DEL	Growth Inhibition Assay			IC50=16.6717 μM	SANGER
GP5d	Growth Inhibition Assay			IC50=17.053 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=17.6294 μM	SANGER
H9	Growth Inhibition Assay			IC50=18.2833 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=18.5119 μM	SANGER
KYSE-150	Growth Inhibition Assay			IC50=18.9986 μM	SANGER
Daoy	Growth Inhibition Assay			IC50=19.5649 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
LB771	Growth Inhibition Assay			IC50=28.8373 μM	SANGER
697	Growth Inhibition Assay			IC50=29.0235 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=29.3748 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=29.3814 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=29.3814 μM	SANGER
L-363	Growth Inhibition Assay			IC50=29.4798 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=29.4901 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=30.4241 μM	SANGER
A2780	Growth Inhibition Assay			IC50=30.7457 μM	SANGER
KU812	Growth Inhibition Assay			IC50=32.3642 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=33.3599 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=33.3889 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=33.6001 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
MOLT-16	Growth Inhibition Assay			IC50=36.952 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
SW982	Growth Inhibition Assay			IC50=38.0998 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=39.3304 μM	SANGER
NB14	Growth Inhibition Assay			IC50=40.7031 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=41.2771 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=41.3063 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
MDA-MB-361	Growth Inhibition Assay			IC50=43.8414 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=43.9532 μM	SANGER
T98G	Growth Inhibition Assay			IC50=44.8517 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=45.6389 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=45.7585 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=47.3791 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=47.9034 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=49.7856 μM	SANGER
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生物活性

製品説明

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.

特性

Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

Targets

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

In Vitro
In vitro	ABT-888 is inactive to SIRT2 (>5 μM). ^[1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ^[2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. ^[3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. ^[4]
Kinase Assay	In vitro PARP assays
Kinase Assay	PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [³H]NAD⁺ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. ^[1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. ^[3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. ^[4]
動物実験	動物モデル	NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
	投与量	~25 mg/kg
	投与経路	Orally administered

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[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

参考

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

+ 展開

化学情報

分子量	244.29	化学式	C₁₃H₁₆N₄O
CAS No.	912444-00-9	SDF	Download Veliparib (ABT-888) SDFをダウンロードする
Smiles	CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 49 mg/mL ( (200.58 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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):