ABT-888 dihydrochloride, also known asVeliparib, is a potent and selective Poly (ADP-Ribose) Polymerase (PARP) Inhibitor. ABT-888 dihydrochloride enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation. ABT-888 dihydrochloride is an orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively).
Chemical Formula: C13H18Cl2N4O
Molecular Weight: 317.214
Elemental Analysis: C, 49.22; H, 5.72; Cl, 22.35; N, 17.66; O, 5.04
ABT 888 dihydrochloride
Chemical Name: 2-[(2R)-2-methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide, dihydrochloride
InChi Code: InChI=1S/C13H16N4O.2ClH/c1-13(6-3-7-15-13)12-16-9-5-2-4-8(11(14)18)10(9)17-12;;/h2,4-5,15H,3,6-7H2,1H3,(H2,14,18)(H,16,17);2*1H/t13-;;/m1../s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
ABT-888 dihydrochloride is inactive to SIRT2 (>5 μM).
ABT-888 dihydrochloride inhibits the PARP activity with EC50 of 2 nM in C41 cells.
ABT-888 dihydrochloride can decrease the PAR levels in both irradiated and nonirradiated H460 cells.
ABT-888 dihydrochloride reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells.
ABT-888 dihydrochloride increases apoptosis and autophagy in H460 cells when combination with radiation.
ABT-888 dihydrochloride inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function.
ABT-888 dihydrochloride (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells.
ABT-888 dihydrochloride shows effective radiosensitivity in oxic H1299 cells. ABT-888 dihydrochloride can attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1.
The oral bioavailability of ABT-888 dihydrochloride is 56%-92% in mice, SD rats, beagle dogs, and cynomolgus monkeys after oral administration. ABT-888 dihydrochloride (25 mg/kg, i.p.) can improve tumor growth delay in a NCI-H460 xenograft model. Combination with radiation, veliparib decreases the tumor vessel formation. ABT-888 dihydrochloride 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 can be maintained over time.
Bhute VJ, Ma Y, Bao X, Palecek SP. The Poly (ADP-Ribose) Polymerase Inhibitor Veliparib and Radiation Cause Significant Cell Line Dependent Metabolic Changes in Breast Cancer Cells. Sci Rep. 2016 Nov 4;6:36061. doi: 10.1038/srep36061. PubMed PMID: 27811964; PubMed Central PMCID: PMC5095763.
Ramalingam SS, Blais N, Mazieres J, Reck M, Jones CM, Juhász E, Urban L, Orlov S, Barlési F, Kio E, Keiholz U, Qin Q, Qian J, Nickner C, Dziubinski J, Xiong H, Ansell P, McKee MD, Giranda V, Gorbunova V. Randomized, Placebo-Controlled, Phase 2 Study of Veliparib in Combination with Carboplatin and Paclitaxel for Advanced/Metastatic Non-Small Cell Lung Cancer. Clin Cancer Res. 2016 Oct 10. pii: clincanres.3069.2016. [Epub ahead of print] PubMed PMID: 27803064.
Munasinghe W, Stodtmann S, Tolcher A, Calvo E, Gordon M, Jalving M, de Vos-Geelen J, Medina D, Bergau D, Nuthalapati S, Hoffman D, Shepherd S, Xiong H. Effect of veliparib (ABT-888) on cardiac repolarization in patients with advanced solid tumors: a randomized, placebo-controlled crossover study. Cancer Chemother Pharmacol. 2016 Nov;78(5):1003-1011. PubMed PMID: 27709282; PubMed Central PMCID: PMC5083757.
Isakoff SJ, Puhalla S, Domchek SM, Friedlander M, Kaufman B, Robson M, Telli ML, Diéras V, Han HS, Garber JE, Johnson EF, Maag D, Qin Q, Giranda VL, Shepherd SP. A randomized Phase II study of veliparib with temozolomide or carboplatin/paclitaxel versus placebo with carboplatin/paclitaxel in BRCA1/2 metastatic breast cancer: design and rationale. Future Oncol. 2016 Oct 14. [Epub ahead of print] PubMed PMID: 27739325.
Chabot P, Hsia TC, Ryu JS, Gorbunova V, Belda-Iniesta C, Ball D, Kio E, Mehta M, Papp K, Qin Q, Qian J, Holen KD, Giranda V, Suh JH. Veliparib in combination with whole-brain radiation therapy for patients with brain metastases from non-small cell lung cancer: results of a randomized, global, placebo-controlled study. J Neurooncol. 2016 Sep 21. [Epub ahead of print] PubMed PMID: 27655223.
Subhash VV, Tan SH, Yeo MS, Yan FL, Peethala PC, Liem N, Krishnan V, Yong WP. ATM expression predicts Veliparib and Irinotecan sensitivity in gastric cancer by mediating P53 independent regulation of cell cycle and apoptosis. Mol Cancer Ther. 2016 Sep 16. pii: molcanther.1002.2015. [Epub ahead of print] PubMed PMID: 27638859.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.