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

Veliparib dihydrochloride  (Synonyms: ABT-888 dihydrochloride)

Cat. No.: HY-10130 Purity: 99.98%
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Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.

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

Veliparib dihydrochloride Chemical Structure

Veliparib dihydrochloride Chemical Structure

CAS No. : 912445-05-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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10 mg USD 84 In-stock
50 mg USD 240 In-stock
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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of Veliparib dihydrochloride:

Veliparib dihydrochloride Related Antibodies

Top Publications Citing Use of Products

32 Publications Citing Use of MCE Veliparib dihydrochloride

Proliferation Assay
WB

    Veliparib dihydrochloride 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 dihydrochloride 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 (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.

    IC50 & Target[1]

    PARP-2

    2.9 nM (Ki)

    PARP-1

    5.2 nM (Ki)

    In Vitro

    Veliparib is inactive to SIRT2 (>5 μM)[1]. Veliparib inhibits the PARP activity with EC50 of 2 nM in C41 cells[2]. Veliparib can decrease the PAR levels in both irradiated and nonirradiated H460 cells. Veliparib reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. Veliparib increases apoptosis and autophagy in H460 cells when combination with radiation[3]. Veliparib inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. Veliparib (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. Veliparib shows effective radiosensitivity in oxic H1299 cells. Veliparib can attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1[4].

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

    Veliparib dihydrochloride Related Antibodies
    In Vivo

    The oral bioavailability of Veliparib is 56%-92% in mice, SD rats, beagle dogs, and cynomolgus monkeys after oral administration[1]. Veliparib (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[3]. Veliparib 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[4].

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

    317.21

    Formula

    C13H18Cl2N4O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 250 mg/mL (788.12 mM; Need ultrasonic)

    DMSO : ≥ 3.2 mg/mL (10.09 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 3.1525 mL 15.7624 mL 31.5249 mL
    5 mM 0.6305 mL 3.1525 mL 6.3050 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    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:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 100 mg/mL (315.25 mM); Clear solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation
    References
    Kinase Assay
    [1]

    PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    For B16F10 syngeneic studies, 6×104 cells are mixed with 50% Matrigel and inoculated by s.c. injection into the flank of 6- to 8-week-old female C57BL/6 mice (20 g). For cisplatin efficacy studies, female nude mice are implanted s.c. by trocar with fragments (20-30 mm3) of human tumors harvested from s.c. grown tumors in nude mice hosts. For the carboplatin and MX-1 cyclophosphamide studies, female scid mice are inoculated with 200 μL of a 1:10 dilution of tumor brei in 45% Matrigel and 45% Spinner MEM. For these established tumor studies, tumors are allowed to grow to the indicated size and then randomized to therapy groups. For DOHH-2 xenograft studies, 1×106 cells are mixed with 50% Matrigel and inoculated by s.c. injection into the flank of male scid mice. Veliparib is delivered by either oral route or continuous infusion using s.c. placement of 14-day Alzet OMP model 2002 in a vehicle containing 0.9% NaCl adjusted to pH 4.0. The OMP delivers at a rate of 12 μL daily and Veliparib doses are calculated accordingly. Temozolomide, cisplatin, carboplatin, and cyclophosphamide are formulated according to the manufacturers' recommendations.

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.1525 mL 15.7624 mL 31.5249 mL 78.8121 mL
    5 mM 0.6305 mL 3.1525 mL 6.3050 mL 15.7624 mL
    10 mM 0.3152 mL 1.5762 mL 3.1525 mL 7.8812 mL
    H2O 15 mM 0.2102 mL 1.0508 mL 2.1017 mL 5.2541 mL
    20 mM 0.1576 mL 0.7881 mL 1.5762 mL 3.9406 mL
    25 mM 0.1261 mL 0.6305 mL 1.2610 mL 3.1525 mL
    30 mM 0.1051 mL 0.5254 mL 1.0508 mL 2.6271 mL
    40 mM 0.0788 mL 0.3941 mL 0.7881 mL 1.9703 mL
    50 mM 0.0630 mL 0.3152 mL 0.6305 mL 1.5762 mL
    60 mM 0.0525 mL 0.2627 mL 0.5254 mL 1.3135 mL
    80 mM 0.0394 mL 0.1970 mL 0.3941 mL 0.9852 mL
    100 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.7881 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Veliparib dihydrochloride 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:

    Veliparib912445-05-7ABT-888ABT888ABT 888PARPAutophagypoly ADP ribose polymeraseInhibitorinhibitorinhibit

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