Veliparib (ABT-888)

製品コードS1004 バッチS100417

印刷

化学情報

Synonyms

NSC 737664

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₃H₁₆N₄O

分子量

244.29

CAS No.

912444-00-9

Solubility (25°C)*

体外

DMSO

49 mg/mL (200.58 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro	Veliparib (ABT-888) is inactive to SIRT2 (>5 μM). ^[1] It inhibits the PARP activity with EC50 of 2 nM in C41 cells. ^[2] This compound could decrease the PAR levels in both irradiated and nonirradiated H460 cells. It also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. Furthermore, it increases apoptosis and autophagy in H460 cells when combination with radiation. ^[3] It also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. At 10 μM, it suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. It shows effective radiosensitivity in oxic H1299 cells. Moreover, it could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. ^[4]
in vivo	Veliparib (ABT-888) has an oral bioavailability of 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys. ^[1] This compound (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, it decreases the tumor vessel formation. ^[3] It 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]
特徴	Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro PARP assays
キナーゼアッセイ	PARP assays for Veliparib (ABT-888) 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.
細胞アッセイ	細胞株	Cell-free assays
	濃度	Ki of 5.2 and 2.9 nM for PARP1 and PARP2
	反応時間
	実験の流れ
動物実験	動物モデル	NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
	投薬量	~25 mg/kg
	投与方法	Orally administered

参考

https://pubmed.ncbi.nlm.nih.gov/17473206/
https://pubmed.ncbi.nlm.nih.gov/19143569/
https://pubmed.ncbi.nlm.nih.gov/17505006/

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2766769/
https://pubmed.ncbi.nlm.nih.gov/19934293/
https://pubmed.ncbi.nlm.nih.gov/17473206/
https://pubmed.ncbi.nlm.nih.gov/22678161/

+ 展开

カスタマーフィードバック

: Data from [Nucl Med Commun, 2011, 32, 1046-1051]

: Data from [Nucl Med Commun, 2011, 32(11), 1046-51]

: Data from [Nucl Med Commun, 2011, 32(11), 1046-51]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

EXO1 as a therapeutic target for Fanconi Anaemia, ZRSR2 and BRCA1-A complex deficient cancers [ Nat Commun, 2025, 16(1):8476]	PubMed: 41006228
CHD6 has poly(ADP-ribose)- and DNA-binding domains and regulates PARP1/2-trapping inhibitor sensitivity via abasic site repair [ Nat Commun, 2025, 16(1):1026]	PubMed: 39863586
PARP7 inhibits type I interferon signaling to prevent autoimmunity and lung disease [ J Exp Med, 2025, 222(5)e20241184]	PubMed: 39969510
Combining Multiplexed CRISPR/Cas9-Nickase and PARP Inhibitors Efficiently and Precisely Targets Cancer Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938]	PubMed: 40327605
ZNF251 haploinsufficiency confers PARP inhibitors resistance in BRCA1-mutated cancer cells through activation of homologous recombination [ Cancer Lett, 2025, 613:217505]	PubMed: 39892701
Role of KLF5 in enhancing ovarian cancer stemness and PARPi resistance: mechanisms and therapeutic targeting [ J Transl Med, 2025, 23(1):492]	PubMed: 40307891
Poly ADP Ribose Polymerase Inhibitors Potentiate Proton Therapy End-of-Range Effects by Accelerating Replication Forks and Promoting Transcription Conflict [ Int J Radiat Oncol Biol Phys, 2025, S0360-3016(25)06197-8]	PubMed: 40882877
PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration-resistant prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70098]	PubMed: 40915979
Homologous Repair-Deficient Pancreatic Cancer: Refined Targeting of DNA Damage Response is an Effective Therapeutic Strategy [ United Eur Gastroent, 2025, 13(7):1328-1342]	PubMed: 40823818
Tousled-like kinase loss confers PARP inhibitor resistance in BRCA1-mutated cancers by impeding non-homologous end joining repair [ Mol Med, 2025, 31(1):18]	PubMed: 39844055

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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