Name | 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide, dihydrochloride salt |
Synonyms | Abt-888 ABT-888 ABT888 HCl ABT-888.2HCl Veliparib 2HCl Veliparib hydrochloride ABT-888 dihydrochloride Veliparib dihydrochloride ABT-888(Veliparib dihydrochloride) 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide dihydrochloride 2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-4-carboxamide dihydrochloride 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide,dihydrochloridesalt 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide, dihydrochloride salt |
CAS | 912445-05-7 |
EINECS | 1592732-453-0 |
InChI | InChI=1/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 |
Molecular Formula | C13H16N4O |
Molar Mass | 244.296 |
Melting Point | >173°C (dec.) |
Solubility | Methanol (Slightly, Heated), THF (Slightly, Heated) |
Appearance | Colorless to white crystalline solid. |
Color | Off-White to Dark Yellow |
Storage Condition | Refrigerator |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.152 ml | 15.762 ml | 31.525 ml |
5 mM | 0.63 ml | 3.152 ml | 6.305 ml |
10 mM | 0.315 ml | 1.576 ml | 3.152 ml |
5 mM | 0.063 ml | 0.315 ml | 0.63 ml |
Overview | veliparib hydrochloride (ABT-888) is an orally effective PARP1/2 inhibitor developed by AbbVie. It was first introduced into clinical practice in 2007. so far, 90 clinical studies have been carried out, including triple negative breast cancer, non-small cell lung cancer, ovarian cancer, melanoma, brain cancer and so on. ABT-888, it was used in combination with DNA-damaging chemotherapeutic drugs to treat glioblastoma multiforme, epithelial ovarian cancer and metastatic brain cancer, and received FDA Orphan Drug Designation in 2008, 2009and 2014 respectively. |
properties | ABT-888 the biggest difference from other PARP inhibitors is that, ABT-888 in combination with chemotherapy drugs in the treatment of tumor in patients with no genotyping, and ABT-888,BMN-673, rekappab et al. were the first to BRCA mutation of tumor patients. Apart from chemotherapy, triple negative breast cancer currently does not have a good targeted therapy, ABT-888 if successful, will be very good to meet the clinical gap. |
pharmacodynamics | According to the results of the study published by AbbVie, ABT-888 was absorbed faster, the peak time (Tmax) of blood drug concentration was 1.2-2.5h;Cmax/AUC increased linearly with the increase of dose, however, the drug has a short half-life of plasma concentration (t1/2=6h) and is rapidly eliminated in vivo, which makes it difficult to maintain the drug concentration required for effective PARP enzyme activity inhibition for a long time, in clinical practice, it is necessary to administer large doses more than twice a day (dosa alone> 400mg/time). |
Use | velipani Dihydrochloride is a poly (ADP-ribose) polymerase (PARP)-1 and -2 inhibitors with Chemical sensitization and antitumor activity. |