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Iniparib (BSI-201) is a potent small-molecule Poly(ADP-ribose) polymerase (PARP1) inhibitor for cancer treatment. Poly(ADP-ribose) polymerase (PARP) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is activated by DNA damage. BSI-201 was the first putative PARP inhibitor to commence phase III clinical trials. Iniparib (BSI-201) produces rapid apoptosis in various cancer cell lines with IC50 values ranging from 40-128 μM and is not toxic in Syrian hamsters at doses as high as 200 mg/kg. BSI-201 was well tolerated and there were no changes in blood counts at the end of treatment. Antitumor activity of Iniparib (BSI-201) was confirmed by Caspace-3 and TUNEL staining of OVCAR-3 tumors. The combination of Iniparib and topotecan produced significant antitumor activity (P<0.001) and increased the percentage of complete tumor regression compared with topotecan alone. In addition, PARP-1 inhibitor BSI-201 may exhibit direct antineoplastic activity against cancers defective in DNA repair.
| Molecular Weight | 292.03 |
| Formula | C7H5IN2O3 |
| CAS Number | 160003-66-7 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PARP Products |
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| 2-Methylquinazolin-4-ol
2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with IC50 of 0.20 mM. |
| DPQ
DPQ is a potent PARP-1 inhibitor. |
| OUL232
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. |
| AZ3391
AZ3391 is a potent inhibitor of PARP. |
| PARP1-IN-5
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). |
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