2. Cell Cycle/DNA Damage Epigenetics Autophagy
  3. PARP Autophagy
  4. Veliparib

Veliparib (ABT-888) est un inhibiteur puissant de PARP, inhibant PARP1 et PARP2 avec Ki des valeurs de 5,2 et 2,9 nM, respectivement.

Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.

For research use only. We do not sell to patients.

Veliparib Chemical Structure

Veliparib Chemical Structure

CAS No. : 912444-00-9

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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of Veliparib:

Veliparib Related Antibodies

Top Publications Citing Use of Products

32 Publications Citing Use of MCE Veliparib

Proliferation Assay
WB

    Veliparib purchased from MedChemExpress. Usage Cited in: J Vet Med Sci. 2018 Nov 23;80(11):1775-1781.  [Abstract]

    PK-15 cells are incubated with 20 μM ABT-888 for 1 hr and subsequently infected with transmissible gastroenteritis virus (TGEV) for 36 hr. Cells are collected and then subjected to Western blot analysis for PARP-1.

    Veliparib purchased from MedChemExpress. Usage Cited in: Electrostatics Joint Conference. 2016 July.

    Dose curve of Veliparib on MDA-MB-231 cells without Electroporation.

    View All PARP Isoform Specific Products:

    View All Isoforms
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively[1].

    IC50 & Target[1]

    PARP-2

    2.9 nM (Ki)

    PARP-1

    5.2 nM (Ki)

    Autophagy

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    133.5 μM
    Compound: ABT-888
    Inhibition of PARP1 in human A549 cells assessed as potentiation of TMZ-mediated cytotoxicity by measuring TMZ IC50 for growth inhibition at 0.5 uM by SRB assay (Rvb TMZ IC50 = 295 uM)
    Inhibition of PARP1 in human A549 cells assessed as potentiation of TMZ-mediated cytotoxicity by measuring TMZ IC50 for growth inhibition at 0.5 uM by SRB assay (Rvb TMZ IC50 = 295 uM)
    		[PMID: 27353531]
    CAPAN-1 IC50
    39.7 μM
    Compound: ABT-888
    Antiproliferative activity against BRCA2 gene mutated human Capan1 cells after 72 hrs by SRB assay
    Antiproliferative activity against BRCA2 gene mutated human Capan1 cells after 72 hrs by SRB assay
    		[PMID: 24398383]
    DLD-1 IC50
    0.75 μM
    Compound: 5
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    		[PMID: 34570508]
    HCC1937 IC50
    97.16 μM
    Compound: ABT-888
    Antiproliferative activity against BRCA1 gene mutated human HCC1937 cells after 72 hrs by SRB assay
    Antiproliferative activity against BRCA1 gene mutated human HCC1937 cells after 72 hrs by SRB assay
    		[PMID: 24398383]
    HCT-116 IC50
    64 μM
    Compound: ABT-888
    Cytotoxicity against human HCT116 cells by SRB assay
    Cytotoxicity against human HCT116 cells by SRB assay
    		[PMID: 27353531]
    Jurkat EC50
    160 μM
    Compound: ABT-888
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay
    		[PMID: 23850199]
    Jurkat EC50
    3 μM
    Compound: ABT-888
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide
    		[PMID: 23850199]
    LoVo EC50
    5.94 nM
    Compound: 1; ABT-888
    Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
    Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
    		[PMID: 26652717]
    LoVo GI50
    6203 nM
    Compound: 1; ABT-888
    Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
    Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
    		[PMID: 26652717]
    MDA-MB-468 EC50
    43 μM
    Compound: Veliparib
    Growth inhibition of human MDA-MB-468 cells after 72 hrs by SRB assay
    Growth inhibition of human MDA-MB-468 cells after 72 hrs by SRB assay
    		[PMID: 27561983]
    Sf9 IC50
    < 10 nM
    Compound: Vel
    Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    		[PMID: 31042381]
    Sf9 IC50
    1.5 nM
    Compound: Vel
    Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    		[PMID: 31042381]
    SW-620 EC50
    27.1 μM
    Compound: Veliparib
    Growth inhibition of human SW620 cells after 72 hrs by SRB assay
    Growth inhibition of human SW620 cells after 72 hrs by SRB assay
    		[PMID: 27561983]
    In Vitro

    Veliparib (ABT-888) is also tested against SIRT2, an enzyme that also uses NAD+ for catalysis, and found to be inactive (>5,000 nM). The receptor profile of Veliparib is determined in a panel of 74 receptor-binding assays at a concentration of 10 μM. 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. The IC50s for these three receptors are 5.3, 1.5, and 1.2 μM, respectively[1].
    c-Met knockdown cells show 4.2- (shMet-A; 95% CI=4-4.5) or 4.6-fold (shMet-B; 95% CI=4.4-4.8) growth inhibition when treated with 60 μM Veliparib (ABT-888). When treated with 38 μM Veliparib, c-Met knockdown cells show 2- (shMet-A; 95% CI=1.5-2.5) or 1.9-fold (shMet-B; 95% CI=1.3-2.5) growth inhibition[2].
    In HaCaT cells, at 6 h post-treatment by Veliparib (ABT-888), cell viability is significantly increases under 1,000 μM sulfur mustard (SM) exposure, whereas Veliparib does not protect cell viability under 100 μM SM exposure. Moreover, the addition of Veliparib no longer shows the protective effect at 24 h post SM exposure[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Veliparib Related Antibodies
    In Vivo

    Veliparib (ABT-888) is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier in syngeneic and xenograft tumor models[1]. In MDA-MB-231 xenograft tumor models, combination treatment (AG014699/PF-02341066 and Veliparib (ABT-888)/Foretinib) substantially reduced tumor growth compared to either inhibitor alone[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    244.29

    Formula

    C13H16N4O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C2NC([C@@]3(NCCC3)C)=NC2=CC=C1)N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 29 mg/mL (118.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0935 mL 20.4675 mL 40.9350 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (8.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (8.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.78%

    SDS (393 KB)

    COA (252 KB) HNMR (211 KB) LCMS (113 KB) Elemental Analysis Report (110 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    PARP1 enzyme activity is measured by using a commercial assay kit with the exception that cell lysates containing wild-type PARP1 or PARP Y907 mutant are used in place of the PARP1 protein included with the kit. Total lysate (500 ng) is added to each reaction. The dose course of PARP inhibitor Veliparib (ABT-888) is from 0.01 to 1,000 μM. PARP enzyme activity of wild-type and mutants is determined after incubation with the substrate is measured using a plate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    Cell viability is quantified using the Cell Counting Kit-8 (CCK-8). This assay is based on Dojindo’s highly water-soluble tetrazolium salt. WST-8 is reduced by dehydrogenases in cells to give an orange, water-soluble formazan dye. The amount of the formazan dye generated by dehydrogenases in cells is directly proportional to the number of living cells. Briefly, exponentially growing HaCaT cells are seeded in 96-well plates at a density of 10,000 cells/well. 6 h or 24 h after exposure to sulfur mustard (SM) and the administration of Veliparib, the CCK-8 reagent is added[3.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    MDA-MB-231 (0.5×106), HCC1937 (2×106) or MCF-7 (5×106) cells are injected into the mammary fat pads of female nude (Swiss Nu/Nu) mice of 6-8 weeks of age. A1034 (0.5×106) cells are injected into the mammary fat pads of female FVB/NJ mice of 6-8 weeks of age. H1993 (0.5×106) cells are injected subcutaneously into the right flank of female nude (Swiss Nu/Nu) mice of 6-8 weeks of age. When the tumor volume reaches 50 mm3, PF-02341066 (5 mg/kg) and Foretinib (5 mg/kg), AG014699 (5 mg/kg) and Veliparib (25 mg/kg), dissolved in aqueous 50 mM sodium acetate, pH 4, are administered to mice five times per week as single agents or in combination for the number of days specified in the figure legend. Tumor is measured at the indicated time points, and tumor volume is calculated by the formula: π/6×length×width2. For MDA-MB-231 and A1034 xenograft mouse models, mice are imaged before and after treatment using the IVIS Imaging System to assess tumor growth. Mice are injected with 100 μL of D-luciferin (15 mg/mL in PBS).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.0935 mL 20.4675 mL 40.9350 mL 102.3374 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 mL 20.4675 mL
    10 mM 0.4093 mL 2.0467 mL 4.0935 mL 10.2337 mL
    15 mM 0.2729 mL 1.3645 mL 2.7290 mL 6.8225 mL
    20 mM 0.2047 mL 1.0234 mL 2.0467 mL 5.1169 mL
    25 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0935 mL
    30 mM 0.1364 mL 0.6822 mL 1.3645 mL 3.4112 mL
    40 mM 0.1023 mL 0.5117 mL 1.0234 mL 2.5584 mL
    50 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
    60 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
    80 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
    100 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0234 mL
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    Veliparib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Veliparib912444-00-9ABT-888ABT888ABT 888PARPAutophagypoly ADP ribose polymeraseInhibitorinhibitorinhibit

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