Veliparib dihydrochloride (also known as ABT888 dihydrochloride; ABT-888 dihydrochloride) is a novel and potent inhibitor of PARP1 and PARP2 [Poly (ADP-Ribose) Polymerase] with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It has chemosensitizing and antitumor activities, and is inactive against SIRT2. ABT-888 has demonstrated excellent in vivo efficacy in a broad spectrum of preclinical tumor models in combination with a variety of cytotoxic agents. ABT-888 is also active on microsatellite instability (MSI) cell lines harboring mutations in both MRE11 and RAD50 genes compared to microsatellite stable (MSS) cell lines (wild-type for both genes). ABT-888 has no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.
理化性质和储存条件
| Molecular Weight (MW) | 317.21 |
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| Formula | C13H18Cl2N4O |
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| CAS No. | 912445-05-7 (Veliparib dihydrochloride) |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: > 3 mg/mL |
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| Water: > 50 mg/mL |
| Ethanol: N/A |
| Other Info | Chemical Name: 2-[(2R)-2-methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide, dihydrochloride
InChi Key: DSBSVDCHFMEYBX-FFXKMJQXSA-N
InChi Code: 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
SMILES Code: O=C(C1=C2C(N=C([C@]3(C)NCCC3)N2)=CC=C1)N.[H]Cl.[H]Cl |
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| Synonyms | NSC 737664 dihydrochloride; NSC737664; NSC-737664 dihydrochloride; ABT888; ABT-888; ABT 888 |
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