An orally bioavailable inhibitor of PARP1 and PARP2
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ABT-888 (hydrochloride)

Item No. 11505

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(2R)-2-methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide, dihydrochloride
CAS Number
912445-05-7
Synonyms
  • Veliparib
Molecular Formula
C13H16N4O • 2HCl
Formula Weight
317.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.25 mg/mlDMSO: 15 mg/mlEthanol: 0.1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
269, 292 nm
SMILES
NC(C1=CC=CC2=C1N=C([C@@]3(NCCC3)C)N2)=O.Cl.Cl
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
InChi Key
DSBSVDCHFMEYBX-FFXKMJQXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $120

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    10 mg

    $157

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    25 mg

    $294

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    Cayman Chemical
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    Product Description

    Poly(ADP-ribose) polymerases (PARPs) have diverse roles in cellular processes, including DNA repair and apoptosis.1,2 ABT-888 is an orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively).3 It enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation.4,5 ABT-888 also acts synergistically with chemotherapies to increase the lethal effects of radiation in cancer cells.6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Davar, D., Beumer, J.H., Hamieh, L., et al. Role of PARP inhibitors in cancer biology and therapy. Curr. Med. Chem. 19(23), 3907-3921 (2012).

    2. Javle, M., and Curtin, N.J. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther. Adv. Med. Oncol. 3(6), 257-267 (2011).

    3. Donawho, C.K., Luo, Y., Penning, T.D., et al. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin. Cancer Res. 13(9), 2728-2737 (2007).

    4. Albert, J.M., Cao, C., Kim, K.W., et al. Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models. Clin. Cancer Res. 13(10), 3033-3042 (2007).

    5. Liu, X., Luo, X., Shi, Y., et al. Poly (ADP-ribose) polymerase activity regulates apoptosis in HeLa cells after alkylating DNA damage. Cancer Biol. Ther. 7(6), 934-941 (2008).

    6. Shelton, J.W., Waxweiler, T.V., Landry, J., et al. In vitro and in vivo enhancement of chemoradiation using the oral PARP inhibitor ABT-888 in colorectal cancer cells. Int. J. Radiat. Oncol. Biol. Phys. 86(3), 469-476 (2013).

    7. Shunkwiler, L., Ferris, G., and Kunos, C. Inhibition of poly(ADP-ribose) polymerase enhances radiochemosensitivity in cancers proficient in DNA double-strand break repair. Int. J. Mol. Sci. 14(2), 3773-3785 (2013).

    Product Citations

    Kremer, D.M., Nelson, B.S., Lin, L., et al. GOT1 inhibition primes pancreatic cancer for ferroptosis through the autophagic release of labile iron. bioRxiv (2020).