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Submit ReviewVeliparib dihydrochloride
Description: High affinity PARP-1 and -2 inhibitor; orally bioavailable
Alternative Names: ABT-888
Chemical Name: 2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-4-carboxamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Veliparib dihydrochloride
Veliparib dihydrochloride is a high affinity PARP-2 and PARP-1 inhibitor (Ki values are 2.9 and 5.2 nM, respectively). Inhibits repair of radiation-induced DNA damage and sensitizes lung cancer cells to radiation. Also increases autophagy and apoptosis in lung cancer cells. Enhances radiation-induced tumor growth delay in mice bearing lung tumor xenografts. Also chemosensitizer. Potentiates effects of temozolomide (Cat. No. 2706) in a mouse melanoma model. Orally bioavailable and brain penetrant.
Compound Libraries for Veliparib dihydrochloride
Veliparib dihydrochloride is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Veliparib dihydrochloride
| M. Wt | 317.21 |
| Formula | C13H16N4O.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 912445-05-7 |
| PubChem ID | 45480520 |
| InChI Key | DSBSVDCHFMEYBX-FFXKMJQXSA-N |
| Smiles | C[C@]1(C2=NC3=CC=CC(C(N)=O)=C3N2)CCCN1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Veliparib dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.72 | 100 | |
| water | 31.72 | 100 |
Preparing Stock Solutions for Veliparib dihydrochloride
The following data is based on the product molecular weight 317.21. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.15 mL | 15.76 mL | 31.52 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.3 mL |
| 10 mM | 0.32 mL | 1.58 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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Product Datasheets for Veliparib dihydrochloride
References for Veliparib dihydrochloride
References are publications that support the biological activity of the product.
Albert et al (2007) Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models. Clin.Cancer Res. 13 3033 PMID: 17505006
Donawho et al (2007) ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin.Cancer Res. 13 2728 PMID: 17473206
If you know of a relevant reference for Veliparib dihydrochloride, please let us know.
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Keywords: Veliparib dihydrochloride, Veliparib dihydrochloride supplier, PARP-1, 2, inhibitors, inhibits, poly(ADP-ribose), polymerase, radiosensitizers, chemosensitizers, high, affinity, orally, bioavailable, brain, penetrant, ABT888, ABT-888, Poly(ADP-ribose), Polymerase, 7026, Tocris Bioscience
1 Citation for Veliparib dihydrochloride
Citations are publications that use Tocris products. Selected citations for Veliparib dihydrochloride include:
Mai et al (2021) NAD+ bioavailability mediates PARG inhibition-induced replication arrest, intra S-phase checkpoint and apoptosis in glioma stem cells. NAR Cancer 3 zcab044 PMID: 34806016
Do you know of a great paper that uses Veliparib dihydrochloride from Tocris? Please let us know.
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Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.