Veliparib(chiral)
2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide
CAS: 912444-00-9
Molecular Formula: C13H16N4O
Veliparib(chiral) - Names and Identifiers
| Name | 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide |
| Synonyms | ABT888 ABT 888 A861695 ABT-888 Veliparib API VELIPARIB UNII-01O4K0631N Veliparib(chiral) ABT-888 (Veliparib, NSC 737664) 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4-carboxamide 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide 2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide 1H-Benzimidazole-4-carboxamide, 2-((2R)-2-methyl-2-pyrrolidinyl)- |
| CAS | 912444-00-9 |
| EINECS | 681-636-1 |
| InChI | InChI=1/C13H16N4O/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)/t13-/m1/s1 |
Veliparib(chiral) - Physico-chemical Properties
| Molecular Formula | C13H16N4O |
| Molar Mass | 244.29 |
| Density | 1.274 |
| Boling Point | 579.0±40.0 °C(Predicted) |
| Flash Point | 303.982°C |
| Solubility | DMSO ≥45mg/mL Water <1.2mg/mL Ethanol <1.2.mg/mL |
| Vapor Presure | 0mmHg at 25°C |
| pKa | 9.22±0.30(Predicted) |
| Storage Condition | 2-8℃ |
| Refractive Index | 1.653 |
| Use | A potent PARP-1/-2 inhibitor shown to potentiate DNA damaging agents |
| In vitro study | ABT-888 effectively inhibit PARP, K I values for PARP-1 and PARP-2 are 5.2 and 2.9 nM, respectively. ABT-888 reduces the survival rate of cloned genes in lung cancer H460 cells and inhibits DNA repair. ABT-888 inhibited C41 cells with an EC50 of 2 nM. The combination of ABT-888 and radiation reduces the formation of tumor blood vessels. |
| In vivo study | ABT-888 delay tumor growth in NCI-H460 xenograft models. ABT-888 inhibited PARP in the B16F10 and 9L xenograft models, thereby enhancing the anticancer activity of temozolomide. The combination of ABT-888 and other cytotoxic agents shows strong anticancer efficacy in MX-1 xenograft models. In A375 and Colo829 transplanted tumor models, according to the tumor size, 3 and 12.5 mg ABT-888 were added per kilogram respectively, and more than 95% PAR in the tumor was inhibited. |
Veliparib(chiral) - Introduction
Veliparib is a potent PARP-1/-2 inhibitor shown to potentiate DNA damaging agents. The ability to potentiate temozolomide (TMZ) and develop a biological marker for PARP inhibition.
Last Update：2022-10-16 17:30:04
Veliparib(chiral) - Reference Information
| biological activity | Veliparib (ABT-888) is a potent inhibitor of PARP1 and parp2, ki was 5.2 nM and 2.9 nM, respectively, inhibiting sirt2. Phase 3. Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2, with Ki of 5.2 nM and 2.9 nM, respectively, in a cell-free assay and no activity against sirt2. Veliparib can increase autophagy and apoptosis. Phase 3. |
| characteristics | ABT-888 enhances the effectiveness of common cancer therapies, such as radiotherapy and alkylating agents. |
| Target | Value |
| PARP2 (Cell-free assay) | 2.9 nM(Ki) |
| PARP1 (Cell-free assay) | 5.2 nM(Ki) |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: Veliparib Visit Supplier Webpage Request for quotationCAS: 912444-00-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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