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Veliparib dihydrochloride

Catalog No. T2105 CAS 912445-05-7

Synonyms: ABT-888 dihydrochloride

Veliparib dihydrochloride (ABT-888 dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2.

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Veliparib dihydrochloride Chemical Structure

Veliparib dihydrochloride, CAS 912445-05-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 67.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 317.00
200 mg	In stock	$ 517.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 98%

Purity: 97.09%

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Description	Veliparib dihydrochloride (ABT-888 dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2.
Targets&IC50	PARP2:2.9 nM(Ki), PARP1:5.2 nM (Ki)
In vitro	Veliparib demonstrates inactivity towards SIRT2 at concentrations greater than 5 μM[1] and exhibits potent inhibition of PARP activity, with an EC50 of 2 nM in C41 cells[2]. It effectively reduces PAR levels in H460 cells, regardless of irradiation status, and significantly impairs clonogenic survival by hindering DNA repair via PARP-1 inhibition. Additionally, when used in conjunction with radiation, Veliparib promotes apoptosis and autophagy in H460 cells[3]. Its ability to inhibit PARP activity extends to H1299, DU145, and 22RV1 cells, a process not influenced by p53 function. At a concentration of 10 μM, Veliparib diminishes the surviving fraction in clonogenic H1299 cells by 43%, enhancing radiosensitivity, particularly in oxygen-rich environments. Furthermore, it reduces the surviving fraction in H1299, DU145, and 22RV1 cells under hypoxic-irradiated conditions[4], confirming its role in sensitizing cancer cells to radiation by targeting PARP-dependent mechanisms.
In vivo	Veliparib exhibits an oral bioavailability ranging from 56% to 92% across different species, including mice, SD rats, beagle dogs, and cynomolgus monkeys[1]. At a dosage of 25 mg/kg (i.p.), it enhances tumor growth delay in NCI-H460 xenograft models and, when combined with radiation, decreases tumor vessel formation[3]. Additionally, Veliparib significantly reduces intratumor PAR levels by over 95% at dosages of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models, with this suppression sustained over time[4].
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.

Synonyms	ABT-888 dihydrochloride
Molecular Weight	317.21
Formula	C13H18Cl2N4O
CAS No.	912445-05-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.2 mg/mL (10.09 mM)

H2O: 50 mg/mL (157.62 mM)

References and Literature

1. Donawho CK, et al. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res. 2007 May 1;13(9):2728-37. 2. Penning TD, et al. Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. J Med Chem. 2009 Jan 22;52(2):514-23. 3. Albert JM, et al. Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models. Clin Cancer Res. 2007 May 15;13(10):3033-42. 4. Robert J. Kinders, et al. Preclinical Modeling of a Phase 0 Clinical Trial: Qualification of a Pharmacodynamic Assay of Poly (ADP-Ribose) Polymerase in Tumor Biopsies of Mouse Xenografts. Clin Cancer Res. Author manuscript; available in PMC 2009 Nov 1.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Autophagy Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cardiovascular Disease Compound Library Anti-Lung Cancer Compound Library Anti-Cancer Compound Library

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Keywords

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