Cat. No. Name Size Price Add Cart
KI0169Veliparib10 mg$192
Veliparib50 mg$592
Veliparib200 mg$1552

Chemical Characteristic

Product NameVeliparib
SynonymsABT-888
CAS No.912444-00-9
Molecular Weight 244.29
FormulaC13H16N4O
Chemical Name(R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide
Smilesc1(nc2c([nH]1)cccc2C(=O)N)[C@@]1(NCCC1)C
Chemical Structure

Biological activities

Veliparib is a novel and potent inhibitor of poly (ADP-ribose) polymerase (PARP) -1 and PARP-2 enzymes with Kis of 5.2 and 2.9 nM, respectively. Veliparib displaces control-specific binding at 50% or greater at the human H1 (61%), the human 5-HT1A (91%), and the human 5-HT7 (84%) sites only, and the IC50 values for these three receptors are 5.3, 1.5, and 1.2 µM, respectively.[1] Veliparib has good oral bioavailability and exhibits a selective biochemical profile and that is unlikely to have adverse effects mediated by a wide range of receptors and ion channels at pharmacologically relevant plasma concentrations.[2] Treating MCF7Tet-On GFP-IBD cells with ionizing radiation (IR) in the presence of veliparib prevents PARP activation and markedly increases residual IRIF (IR-induced foci) at 3 and 24 hours. Besides, veliparib blocks IRIF resolution and cell proliferation , driving tumor cells toward accelerated senescence and suppressing tumor regrowth compared with IR alone.[3] Meanwhile, veliparib displays excellent potency in a C41 whole cell assay with an EC50 of 2 nM.[4] Veliparib strongly potentiates temozolomide in the B16F10 s.c. murine melanoma model. Veliparib at doses as low as 3.1 mg/kg/d and a maximal efficacy achieved at 25 mg/kg/d dramatically increases the efficacy of temozolomide. In the MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation), veliparib potentiates cisplatin, carboplatin, and cyclophosphamide, causing regression of established tumors. [1] A phase 0 clinical study of veliparib shows the statistically significant inhibition of PARP activity in tumor biopsy specimens and peripheral blood mononuclear cells at a single oral dose of 25 or 50 mg. [2] In B16F10 melanoma and MX-1 breast cancer models, veliparib demonstrates significant efficacy in combination with a variety of cytotoxic agents, including temozolomide, carboplatin, and cyclophosphamide.[4]

Protocols

Veliparib is diluted in DMSO. [1]

References

[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, 13(9): 2728-2737.
[2] Li X, et al. Disposition and drug-drug interaction potential of veliparib (ABT-888), a novel and potent inhibitor of poly (ADP-ribose) polymerase. Drug Metab Dispos. 2011, 39(7):1161-1169.
[3] Efimova EV, et al. Poly (ADP-ribose) polymerase inhibitor induces accelerated senescence in irradiated breast cancer cells and tumors. Cancer Res. 2010, 70(15): 6277-6282.
[4] Penning TD, et al. Discovery of the Poly (ADP-ribose) polymerase (PARP) inhibitor2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. J Med Chem. 2009, 52(2): 514-523.
[5] 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, 13(10): 3033-3042.
[6] Clarke MJ, et al. Effective sensitization of temozolomide by Veliparib is lost with development of temozolomide resistance in glioblastoma xenograft lines. Mol Cancer Ther. 2009, 8(2): 407-414.
[7] Kinders RJ, 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. 2008, 14(21): 6877-6885.

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