Veliparib dihydrochloridePARP-1/PARP-2 inhibitor CAS# 912445-05-7 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 912445-05-7 | SDF | Download SDF |
| PubChem ID | 45480520 | Appearance | Powder |
| Formula | C13H18Cl2N4O | M.Wt | 317.21 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ABT-888 dihydrochloride | ||
| Solubility | H2O : ≥ 50 mg/mL (157.62 mM) DMSO : ≥ 3.2 mg/mL (10.09 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide;dihydrochloride | ||
| SMILES | CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N.Cl.Cl | ||
| Standard InChIKey | DSBSVDCHFMEYBX-FFXKMJQXSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. | |||||
| Targets | PARP1 | PARP2 | ||||
| IC50 | 5.2 nM (Ki) | 2.9 nM (Ki) | ||||
Veliparib dihydrochloride Dilution Calculator
Veliparib dihydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1525 mL | 15.7624 mL | 31.5249 mL | 63.0497 mL | 78.8121 mL |
| 5 mM | 0.6305 mL | 3.1525 mL | 6.305 mL | 12.6099 mL | 15.7624 mL |
| 10 mM | 0.3152 mL | 1.5762 mL | 3.1525 mL | 6.305 mL | 7.8812 mL |
| 50 mM | 0.063 mL | 0.3152 mL | 0.6305 mL | 1.261 mL | 1.5762 mL |
| 100 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.6305 mL | 0.7881 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Veliparib dihydrochloride is a potent inhibitor of PARP-1 and PARP-2 with K (i) s of 5.2 and 2.9 nmol/L, respectively [1].
PARP is short of poly ADP ribose polymerase and is reported as an overexpressed enzyme in a variety of cancers. Since it has been revealed that several forms of cancer more independent on PARP compared with regular cells, which making PARP as an attractive target for cancer therapy. Many studies have shown that PARP inhibitors act as radio- and chemotherapy- sensitizers in preclinical studies using both in vitro and in vivo models [2] [3].
Veliparib dihydrochloride is a selective inhibitor of PARP. When tested with colon cancer cell lines HCT-116 and HT-29, using veliparib dihydrochloride as an adjuvant and combing with SN38 or Oxall resulted in increasing G2/M cell cycle arrest and increased levels of DNA damage via inhibiting PARP-1 and PARP-2 [4].
In mouse model with B16F10 murine melanoma cells injected subcutaneously, oral administration of veliparib dihydrochloride with temozolomide increased the efficacy at the concentration of 3.1 mg/kg/d~25 mg/kg/d and markedly slowed tumor progression. And similar results were achieved when tested with MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation) or HCT-116 colon carcinoma model [1].
References:
[1]. Donawho, C.K., et al., ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res, 2007. 13(9): p. 2728-37.
[2]. Benafif, S. and M. Hall, An update on PARP inhibitors for the treatment of cancer. Onco Targets Ther, 2015. 8: p. 519-28.
[3]. Guillot, C., et al., PARP inhibition and the radiosensitizing effects of the PARP inhibitor ABT-888 in in vitro hepatocellular carcinoma models. BMC Cancer, 2014. 14: p. 603.
[4]. Davidson, D., et al., The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines. Invest New Drugs, 2013. 31(2): p. 461-8.
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Dynamic regulation of Rad51 by E2F1 and p53 in prostate cancer cells upon drug-induced DNA damage under hypoxia.[Pubmed:24627085]
Mol Pharmacol. 2014 Jun;85(6):866-76.
Intratumoral hypoxia has been proposed to create a "mutator" phenotype through downregulation of DNA repair, leading to increased genomic instability and drug resistance. Such downregulation of DNA repair has been proposed to sensitize hypoxic cancer cells to DNA-damaging agents and inhibitors of DNA repair. Here, we showed that prostate cancer cells with mutant p53 were resistant to the poly(ADP-ribose) polymerase inhibitor, veliparib (2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide, dihydrochloride; Abbott Laboratories, Abbott Park, IL), and the DNA-damaging topoisomerase I inhibitor camptothecin-11 (CPT-11) or SN38 (7-ethyl-10-hydroxycamptothecin) under hypoxia. Upregulation of Rad51 by E2F1 upon DNA damage under hypoxia contributed to such resistance, which was reversed by either inhibiting RAD51 transcription with small interfering RNA or by expressing wild-type p53 in the p53 null prostate cancer line. Accumulation of endogenous p53 but not E2F1 and suppressed RAD51 transcription was observed in prostate cancer line with wild-type p53 after DNA damage under hypoxia. Combining veliparib with CPT-11 significantly enhanced DNA damage and apoptosis under both hypoxic and normoxic culture conditions. Such enhanced DNA damage and antitumor activities were seen in the presence of Rad51 upregulation and confirmed in vivo with PC3 mouse xenografts. These data illustrate a dynamic regulation of Rad51 by E2F1 and p53 in prostate cancer cells' response to hypoxia and DNA damage. The veliparib and CPT-11 combination can be further explored as a treatment of metastatic castration-resistant prostate cancers that have frequent p53 mutations and enriched genomic instability.
