2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide Basic information
Abstract Biological activity In vitro In vivo Features References
Product Name: 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide
Synonyms: 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide;1H-Benzimidazole-4-carboxamide, 2-((2R)-2-methyl-2-pyrrolidinyl)-;2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide;A861695;2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide;Veliparib;ABT-888,Veliparib;Veliparib(chiral)
CAS: 912444-00-9
MF: C13H16N4O.2ClH
MW: 317.218
EINECS:
Product Categories: Amines;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitor;PARP
Mol File: 912444-00-9.mol
2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-
carboxamide Structure
2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide Chemical Properties
density 1.274
Safety Information
MSDS Information
2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide Usage And Synthesis
Abstract Veliparib (ABT-888) is a potential anti-cancer drug acting as a PARP inhibitor. It kills cancer cells by blocking a protein called PARP, thereby preventing the repair of DNA or genetic damage in cancer cells and possibly making them more susceptible to anticancer treatments.
Veliparib (ABT-888) is being investigated to treat squamous and non-squamous non-small cell lung cancer, BRCA breast cancer, triple negative breast cancer and ovarian cancer.
Biological activity Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.
In vitro Veliparib (ABT-888) is a potential anti-cancer drug acting as a PARP inhibitor,which inhibits PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays,respectively.ABT-888 reduces clonogenic survival and inhibits DNA repair in H460 cells. ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells.
In vivo ABT-888 inhibits PARP in B16F10 and 9L xenograft models, thus enhancing the anticancer activity of temozolomide. The Combined with other cytotoxic agents, ABT-888 shows strong antitumor effect in MX-1 xenograft model. ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg according to the the size of tumors in A375 and Colo829 xenograft models.
Features ABT-888 enhances the effectiveness of common cancer treatments, such as radiation therapy and alkylating agents.
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Chemical Properties Off-White Solid
Uses ABT-888 is a potent, orally bioavailable PARP-1/-2 inhibitor shown to potentiate DNA damaging agents. The ability to potentiate temozolomide (TMZ) and develop a biological marker for PARP inhibition was evaluated in vivo.
Definition ChEBI: A benzimidazole substituted with a carbamoyl group at C-4 and a (2R)-2-methylpyrrolidin-2-yl moiety at C-2. It is a potent, orally bioavailable PARP inhibitor.
2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide Preparation Products And Raw materials