1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. PARP Autophagy
  3. 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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 912444-00-9

Tamaño Precio Stock Cantidad
Muestra gratis (0.1 - 0.2 mg)   Solicite ahora  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg En stock
500 mg   Obtener un presupuesto  
1 g   Obtener un presupuesto  

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Revisión del cliente

Based on 49 publication(s) in Google Scholar

Other Forms of Veliparib:

Top Publications Citing Use of Products

49 Publications Citing Use of MCE Veliparib

Cell Proliferation/Viability Assay
WB
RT-PCR
Bio/Physico-chemical Assay

    Veliparib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 16:e15585.  [Abstract]

    Veliparib (0-100 μM; 72 h). Dose‐response curves for Veliparib after 72 h of treatment in MDA‐MB‐468 cells comparing empty vector control (Control) and ARID1B OE cells.

    Veliparib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 24;12(1):3931.  [Abstract]

    Veliparib (10 μM; 24 h). Immunoblots for STAT1a S727p in iBMDMs treated with IFNγ ± Veliparib (Vel.) as indicated.

    Veliparib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 24;12(1):3931.  [Abstract]

    Veliparib (10 μM; 24 h). Bar graphs showing the relative mRNA levels upon treatment IFNγ treatment ± Veliparib (Vel.).

    Veliparib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 24;12(1):3931.  [Abstract]

    Veliparib (10 μM; 24 h). PARP catalytic inhibition results in attenuation of NOS activity in iBMDMs. The cells were treated with IFNγ and Veliparib for 24 hours as indicated.

    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.
    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    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 3
    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]
    A549 IC50
    133.5 3
    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 3
    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]
    CAPAN-1 EC50
    >10 3
    Compound: 1; ABT-888
    Cytotoxicity against BRCA2-deficient human Capan1 cells
    Cytotoxicity against BRCA2-deficient human Capan1 cells
    [PMID: 26652717]
    DLD-1 IC50
    0.75 3
    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]
    CAPAN-1 IC50
    39.7 3
    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]
    HCC1937 IC50
    97.16 3
    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]
    Sf9 IC50
    1.5 1
    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]
    HCT-116 IC50
    64 3
    Compound: ABT-888
    Cytotoxicity against human HCT116 cells by SRB assay
    Cytotoxicity against human HCT116 cells by SRB assay
    [PMID: 27353531]
    A549 IC50
    133.5 3
    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]
    DLD-1 IC50
    0.75 3
    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]
    Jurkat EC50
    160 3
    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]
    DLD-1 IC50
    69 3
    Compound: Veliparib
    Cytotoxicity against human DLD-1 cells expressing BRCA2 assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    Cytotoxicity against human DLD-1 cells expressing BRCA2 assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    [PMID: 37484567]
    A549 IC50
    15.22 3
    Compound: ABT-888
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 38554475]
    Jurkat EC50
    3 3
    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]
    DLD-1 IC50
    8.85 3
    Compound: Veliparib
    Cytotoxicity against human DLD-1 cells with BRCA2 knockout assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    Cytotoxicity against human DLD-1 cells with BRCA2 knockout assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    [PMID: 37484567]
    A549 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    LoVo EC50
    5.94 1
    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]
    HCC1937 IC50
    97.16 3
    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]
    LoVo GI50
    6203 1
    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]
    LoVo EC50
    5.94 1
    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]
    MDA-MB-468 EC50
    43 3
    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]
    HCT-116 IC50
    64 3
    Compound: ABT-888
    Cytotoxicity against human HCT116 cells by SRB assay
    Cytotoxicity against human HCT116 cells by SRB assay
    [PMID: 27353531]
    Sf9 IC50
    < 10 1
    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]
    Jurkat EC50
    160 3
    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]
    Sf9 IC50
    1.5 1
    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]
    Jurkat EC50
    3 3
    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]
    SW-620 EC50
    27.1 3
    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]
    MDA-MB-468 EC50
    43 3
    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]
    CAPAN-1 EC50
    > 10000 1
    Compound: 1; ABT-888
    Cytotoxicity against BRCA2-deficient human Capan1 cells
    Cytotoxicity against BRCA2-deficient human Capan1 cells
    [PMID: 26652717]
    CAPAN-1 IC50
    39.7 3
    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]
    MRC5 EC50
    >10 3
    Compound: 1; ABT-888
    Cytotoxicity against human MRC5 cells
    Cytotoxicity against human MRC5 cells
    [PMID: 26652717]
    DLD-1 IC50
    0.75 3
    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]
    SW-620 EC50
    27.1 3
    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]
    DLD-1 IC50
    69 3
    Compound: Veliparib
    Cytotoxicity against human DLD-1 cells expressing BRCA2 assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    Cytotoxicity against human DLD-1 cells expressing BRCA2 assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    [PMID: 37484567]
    LoVo GI50
    6203 1
    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]
    DLD-1 IC50
    8.85 3
    Compound: Veliparib
    Cytotoxicity against human DLD-1 cells with BRCA2 knockout assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    Cytotoxicity against human DLD-1 cells with BRCA2 knockout assessed as reduction in cell proliferation incubated for 5 days by sulforhodamine B analysis
    [PMID: 37484567]
    Sf9 IC50
    <10 1
    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]
    FaDu IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human FaDu cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human FaDu cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    HCC1937 IC50
    97.16 3
    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 3
    Compound: ABT-888
    Cytotoxicity against human HCT116 cells by SRB assay
    Cytotoxicity against human HCT116 cells by SRB assay
    [PMID: 27353531]
    HGC-27 IC50
    16.03 3
    Compound: ABT-888
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 38554475]
    HH IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human HH cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human HH cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    HL-60 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    HUVEC IC50
    > 100 3
    Compound: Veliparib
    Inhibition of cell proliferation in HUVECs
    Inhibition of cell proliferation in HUVECs
    [PMID: 38678823]
    HeLa IC50
    18.11 3
    Compound: ABT-888
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 38554475]
    HepG2 IC50
    13.69 3
    Compound: ABT-888
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 38554475]
    Jurkat EC50
    160 3
    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 3
    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]
    K562 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    LoVo EC50
    5.94 1
    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 1
    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]
    MCF7 IC50
    > 100 3
    Compound: Veliparib
    Inhibition of cell proliferation in human MCF7 cells
    Inhibition of cell proliferation in human MCF7 cells
    [PMID: 38678823]
    MDA-MB-231 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    MDA-MB-436 IC50
    > 100 3
    Compound: Veliparib
    Inhibition of cell proliferation in human MDA-MB-436 cells assessed as PARP trapping effect
    Inhibition of cell proliferation in human MDA-MB-436 cells assessed as PARP trapping effect
    [PMID: 38678823]
    MDA-MB-468 EC50
    43 3
    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]
    MOLT-4 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    MRC5 EC50
    > 10 3
    Compound: 1; ABT-888
    Cytotoxicity against human MRC5 cells
    Cytotoxicity against human MRC5 cells
    [PMID: 26652717]
    PC-3 IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    SW-620 EC50
    27.1 3
    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]
    Sf9 IC50
    1.5 1
    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]
    Sf9 IC50
    < 10 1
    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]
    SiHa IC50
    > 10 3
    Compound: VI
    Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth by MTT assay
    [PMID: 38776806]
    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.

    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.

    Ensayo clínico
    Peso molecular

    244.29

    Fòrmula

    C13H16N4O

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvente y solubilidad
    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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Pureza y Documentación

    Purity: 99.77%

    Referencias
    Ensayo de quinasas
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Ensayo celular
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Administraciòn de animales
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Referencias

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    Productos vistos recientemente:

    Consulta en línea

    Your information is safe with us. * Required Fields.

    Nombre del producto

     

    Requested Quantity *

    Nombre del solicitante *

     

    Saludo

    Direcciòn del E-mail *

     

    Número de teléfono *

    Department

     

    Nombre de la Organizaciòn *

    City

    Provincia

    Country or Region *

         

    Observaciones

    Consulta para venta a granel

    Inquiry Information

    Nombre del producto:
    Veliparib
    Cat. No.:
    HY-10129
    Cantidad:
    MCE Japan Authorized Agent: