Veliparib free base
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MedKoo CAT#: 203115

CAS#: 912444-00-9 (free base)

Description: Veliparib, also known as ABT-888, is a poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.


Chemical Structure

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Veliparib free base
CAS# 912444-00-9 (free base)

Theoretical Analysis

MedKoo Cat#: 203115
Name: Veliparib free base
CAS#: 912444-00-9 (free base)
Chemical Formula: C13H16N4O
Exact Mass: 244.13241
Molecular Weight: 244.29
Elemental Analysis: C, 63.91; H, 6.60; N, 22.93; O, 6.55

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1350.0 Ready to ship
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Related CAS #: 912444-00-9 (free base)   912445-05-7 (HCl)  

Synonym: ABT888; ABT-888; ABT 888; Veliparib

IUPAC/Chemical Name: (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

InChi Key: JNAHVYVRKWKWKQ-CYBMUJFWSA-N

InChi Code: InChI=1S/C13H16N4O/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)/t13-/m1/s1

SMILES Code: O=C(C1=C2C(NC([C@]3(C)NCCC3)=N2)=CC=C1)N

Appearance: White to off-white 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, not in water

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

Biological target: Veliparib (ABT-888) inhibits PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
In vitro activity: The effects of DNA damage repair inhibitor Veliparib in combination with artesunate (AS) on hydatid cysts was evaluated in vitro. Protoscoleces of E. granulosus (E.g PSCs) were incubated with low AS (AS-L, 65 μM), moderate AS (AS-M, 130 μM), and high AS (AS-H, 325 μM), AS-L/M/H+Veliparib (10 μM), and ABZ (25 μM), respectively. The AS-H+Veliparib group showed the maximal protoscolicidal effects. Ultrastructural change revealed that germinal layer (GL) cells were reduced, and lipid droplets appeared. AS could induce DNA injuries in PSCs. The 8-OHdG was expressed in the PSCs and GL of the cysts in mice, especially in the presence of Veliparib. The most severe DNA damages were observed in the AS-H+Veliparib group. Meanwhile, the expression of ribosomal protein S9 (RPS9) gene in the AS-H+Veliparib group was significantly lower than that in the AS-H group. Reference: Dis Markers. 2020 Jul 1;2020:8259820. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355356/
In vivo activity: The in vivo efficacy of ABT-888 was evaluated in syngeneic and xenograft models in combination with temozolomide, platinums, cyclophosphamide, and ionizing radiation. ABT-888 strongly potentiated temozolomide in the B16F10 s.c. murine melanoma model. PARP inhibition dramatically increased the efficacy of temozolomide at ABT-888 doses as low as 3.1 mg/kg/d and a maximal efficacy achieved at 25 mg/kg/d. In the 9L orthotopic rat glioma model, temozolomide alone exhibited minimal efficacy, whereas ABT-888, when combined with temozolomide, significantly slowed tumor progression. In the MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation), ABT-888 potentiated cisplatin, carboplatin, and cyclophosphamide, causing regression of established tumors, whereas with comparable doses of cytotoxic agents alone, only modest tumor inhibition was exhibited. Finally, ABT-888 potentiated radiation (2 Gy/d x 10) in an HCT-116 colon carcinoma model. In each model, ABT-888 did not display single-agent activity. Reference: Clin Cancer Res. 2007 May 1;13(9):2728-37. https://clincancerres.aacrjournals.org/content/13/9/2728.long

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.0 126.9
DMF 0.25 1.02
Ethanol 0.1 0.41
PBS (pH 7.2) 10.0 40.93

Preparing Stock Solutions

The following data is based on the product molecular weight 244.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE, Ferguson DC, Ghoreishi-Haack NS, Grimm DR, Guan R, Han EK, Holley-Shanks RR, Hristov B, Idler KB, Jarvis K, Johnson EF, Kleinberg LR, Klinghofer V, Lasko LM, Liu X, Marsh KC, McGonigal TP, Meulbroek JA, Olson AM, Palma JP, Rodriguez LE, Shi Y, Stavropoulos JA, Tsurutani AC, Zhu GD, Rosenberg SH, Giranda VL, Frost DJ. 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. doi: 10.1158/1078-0432.CCR-06-3039. PMID: 17473206. 2. Li YF, Wen LM, Zhao J, Lv GD, Lu S, Lu S, Zheng X, Chen B, Tian CY, Gong YH, Gao HJ, Wang JH. In Vitro and In Vivo Efficacy of DNA Damage Repair Inhibitor Veliparib in Combination with Artesunate against Echinococcus granulosus. Dis Markers. 2020 Jul 1;2020:8259820. doi: 10.1155/2020/8259820. PMID: 32714467; PMCID: PMC7355356.
In vitro protocol: 1. Li YF, Wen LM, Zhao J, Lv GD, Lu S, Lu S, Zheng X, Chen B, Tian CY, Gong YH, Gao HJ, Wang JH. In Vitro and In Vivo Efficacy of DNA Damage Repair Inhibitor Veliparib in Combination with Artesunate against Echinococcus granulosus. Dis Markers. 2020 Jul 1;2020:8259820. doi: 10.1155/2020/8259820. PMID: 32714467; PMCID: PMC7355356.
In vivo protocol: 1. Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE, Ferguson DC, Ghoreishi-Haack NS, Grimm DR, Guan R, Han EK, Holley-Shanks RR, Hristov B, Idler KB, Jarvis K, Johnson EF, Kleinberg LR, Klinghofer V, Lasko LM, Liu X, Marsh KC, McGonigal TP, Meulbroek JA, Olson AM, Palma JP, Rodriguez LE, Shi Y, Stavropoulos JA, Tsurutani AC, Zhu GD, Rosenberg SH, Giranda VL, Frost DJ. 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. doi: 10.1158/1078-0432.CCR-06-3039. PMID: 17473206. 2. Li YF, Wen LM, Zhao J, Lv GD, Lu S, Lu S, Zheng X, Chen B, Tian CY, Gong YH, Gao HJ, Wang JH. In Vitro and In Vivo Efficacy of DNA Damage Repair Inhibitor Veliparib in Combination with Artesunate against Echinococcus granulosus. Dis Markers. 2020 Jul 1;2020:8259820. doi: 10.1155/2020/8259820. PMID: 32714467; PMCID: PMC7355356.

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1: 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.

2: 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.

3: 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.

4: 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.

5: 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.

6: 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.

7: Pratz KW, Rudek MA, Gojo I, Litzow MR, McDevitt MA, Ji JJ, Karnitz L, Herman JG, Kinders R, Smith BD, Gore SD, Carraway H, Showel MM, Gladstone DE, Levis MJ, Tsai HL, Rosner GL, Chen A, Kaufmann SH, Karp J. A Phase I study of topotecan, carboplatin and the PARP inhibitor veliparib in acute leukemias, aggressive myeloproliferative neoplasms and chronic myelomonocytic leukemia. Clin Cancer Res. 2016 Aug 22. pii: clincanres.1274.2016. [Epub ahead of print] PubMed PMID: 27551000.

8: Gojo I, Beumer JH, Pratz KW, McDevitt MA, Baer MR, Blackford AL, Smith BD, Gore SD, Carraway H, Showel MM, Levis MJ, Dezern A, Gladstone DE, Ji JJ, Wang L, Kinders R, Pouquet M, Ali-Walbi I, Rudek MA, Poh W, Herman JG, Karnitz L, Kaufmann SH, Chen A, Karp J. A phase 1 study of the PARP inhibitor veliparib in combination with temozolomide in acute myeloid leukemia. Clin Cancer Res. 2016 Aug 8. pii: clincanres.0984.2016. [Epub ahead of print] PubMed PMID: 27503200.

9: Rugo HS, Olopade OI, DeMichele A, Yau C, van 't Veer LJ, Buxton MB, Hogarth M, Hylton NM, Paoloni M, Perlmutter J, Symmans WF, Yee D, Chien AJ, Wallace AM, Kaplan HG, Boughey JC, Haddad TC, Albain KS, Liu MC, Isaacs C, Khan QJ, Lang JE, Viscusi RK, Pusztai L, Moulder SL, Chui SY, Kemmer KA, Elias AD, Edmiston KK, Euhus DM, Haley BB, Nanda R, Northfelt DW, Tripathy D, Wood WC, Ewing C, Schwab R, Lyandres J, Davis SE, Hirst GL, Sanil A, Berry DA, Esserman LJ; I-SPY 2 Investigators.. Adaptive Randomization of Veliparib-Carboplatin Treatment in Breast Cancer. N Engl J Med. 2016 Jul 7;375(1):23-34. doi: 10.1056/NEJMoa1513749. PubMed PMID: 27406347.

10: Kummar S, Wade JL, Oza AM, Sullivan D, Chen AP, Gandara DR, Ji J, Kinders RJ, Wang L, Allen D, Coyne GO, Steinberg SM, Doroshow JH. Randomized phase II trial of cyclophosphamide and the oral poly (ADP-ribose) polymerase inhibitor veliparib in patients with recurrent, advanced triple-negative breast cancer. Invest New Drugs. 2016 Jun;34(3):355-63. doi: 10.1007/s10637-016-0335-x. PubMed PMID: 26996385; PubMed Central PMCID: PMC4860030.

11: Villalona-Calero MA, Duan W, Zhao W, Shilo K, Schaaf LJ, Thurmond J, Westman JA, Marshall J, Xiaobai L, Ji J, Rose J, Lustberg M, Bekaii-Saab T, Chen A, Timmers C. Veliparib Alone or in Combination with Mitomycin C in Patients with Solid Tumors With Functional Deficiency in Homologous Recombination Repair. J Natl Cancer Inst. 2016 Feb 4;108(7). pii: djv437. doi: 10.1093/jnci/djv437. PubMed PMID: 26848151; PubMed Central PMCID: PMC4948564.

12: LoRusso PM, Li J, Burger A, Heilbrun LK, Sausville EA, Boerner SA, Smith D, Pilat MJ, Zhang J, Tolaney SM, Cleary JM, Chen AP, Rubinstein L, Boerner JL, Bowditch A, Cai D, Bell T, Wolanski A, Marrero AM, Zhang Y, Ji J, Ferry-Galow K, Kinders RJ, Parchment RE, Shapiro GI. Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor Veliparib (ABT-888) in Combination with Irinotecan in Patients with Advanced Solid Tumors. Clin Cancer Res. 2016 Jul 1;22(13):3227-37. doi: 10.1158/1078-0432.CCR-15-0652. PubMed PMID: 26842236; PubMed Central PMCID: PMC4930710.

13: Bogliolo S, Cassani C, Dominoni M, Musacchi V, Venturini PL, Spinillo A, Ferrero S, Gardella B. Veliparib for the treatment of ovarian cancer. Expert Opin Investig Drugs. 2016;25(3):367-74. doi: 10.1517/13543784.2016.1146677. Review. PubMed PMID: 26807493.

14: Rodler ET, Kurland BF, Griffin M, Gralow JR, Porter P, Yeh RF, Gadi VK, Guenthoer J, Beumer JH, Korde L, Strychor S, Kiesel BF, Linden HM, Thompson JA, Swisher E, Chai X, Shepherd S, Giranda V, Specht JM. Phase I Study of Veliparib (ABT-888) Combined with Cisplatin and Vinorelbine in Advanced Triple-Negative Breast Cancer and/or BRCA Mutation-Associated Breast Cancer. Clin Cancer Res. 2016 Jun 15;22(12):2855-64. doi: 10.1158/1078-0432.CCR-15-2137. PubMed PMID: 26801247; PubMed Central PMCID: PMC4911292.

15: Landrum LM, Brady WE, Armstrong DK, Moore KN, DiSilvestro PA, O'Malley DM, Tenney ME, Rose PG, Fracasso PM. A phase I trial of pegylated liposomal doxorubicin (PLD), carboplatin, bevacizumab and veliparib in recurrent, platinum-sensitive ovarian, primary peritoneal, and fallopian tube cancer: An NRG Oncology/Gynecologic Oncology Group study. Gynecol Oncol. 2016 Feb;140(2):204-9. doi: 10.1016/j.ygyno.2015.11.024. PubMed PMID: 26616225; PubMed Central PMCID: PMC4724478.

16: Gupta SK, Kizilbash SH, Carlson BL, Mladek AC, Boakye-Agyeman F, Bakken KK, Pokorny JL, Schroeder MA, Decker PA, Cen L, Eckel-Passow JE, Sarkar G, Ballman KV, Reid JM, Jenkins RB, Verhaak RG, Sulman EP, Kitange GJ, Sarkaria JN. Delineation of MGMT Hypermethylation as a Biomarker for Veliparib-Mediated Temozolomide-Sensitizing Therapy of Glioblastoma. J Natl Cancer Inst. 2015 Nov 27;108(5). pii: djv369. doi: 10.1093/jnci/djv369. PubMed PMID: 26615020; PubMed Central PMCID: PMC4862419.

17: Gabrielson A, Tesfaye AA, Marshall JL, Pishvaian MJ, Smaglo B, Jha R, Dorsch-Vogel K, Wang H, He AR. Phase II study of temozolomide and veliparib combination therapy for sorafenib-refractory advanced hepatocellular carcinoma. Cancer Chemother Pharmacol. 2015 Nov;76(5):1073-9. doi: 10.1007/s00280-015-2852-2. PubMed PMID: 26449224; PubMed Central PMCID: PMC4612326.

18: Mizugaki H, Yamamoto N, Nokihara H, Fujiwara Y, Horinouchi H, Kanda S, Kitazono S, Yagishita S, Xiong H, Qian J, Hashiba H, Shepherd SP, Giranda V, Tamura T. A phase 1 study evaluating the pharmacokinetics and preliminary efficacy of veliparib (ABT-888) in combination with carboplatin/paclitaxel in Japanese subjects with non-small cell lung cancer (NSCLC). Cancer Chemother Pharmacol. 2015 Nov;76(5):1063-72. doi: 10.1007/s00280-015-2876-7. PubMed PMID: 26433581; PubMed Central PMCID: PMC4612330.

19: VanderWeele DJ, Paner GP, Fleming GF, Szmulewitz RZ. Sustained Complete Response to Cytotoxic Therapy and the PARP Inhibitor Veliparib in Metastatic Castration-Resistant Prostate Cancer - A Case Report. Front Oncol. 2015 Jul 22;5:169. doi: 10.3389/fonc.2015.00169. PubMed PMID: 26258074; PubMed Central PMCID: PMC4510409.

20: Wagner LM. Profile of veliparib and its potential in the treatment of solid tumors. Onco Targets Ther. 2015 Jul 29;8:1931-9. doi: 10.2147/OTT.S69935. Review. PubMed PMID: 26251615; PubMed Central PMCID: PMC4524591.