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Enzymes for Research, Diagnostic and Industrial Use

Iniparib (BSI-201)

Cat No.
CEI-0328
Description
As a competitive ATP inhibitor, BSI-201(iniparib) is one of the most specific and effective C-nitroso-derivative PARP1 inhibitor.
Alias
SAR240550
CAS No.
160003-66-7
Molecular Weight
292.03
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
SAR240550
Targets
PARP
Molecular Formula
C7H5IN2O3
Chemical Name
4-iodo-3-nitrobenzamide
Solubility
DMSO 58 mg/mL Water
In vitro
As a competitive ATP inhibitor, BSI-201(iniparib) is one of the most specific and effective C-nitroso-derivative PARP1 inhibitor. In breast and ovarian carcinomas that harbor BRCA2 mutations, BSI-201(iniparib) shows inhibition to those cell lines. Iniparib nonselectively modifies cysteine-containing proteins in tumor cells, and the primary mechanism of action for iniparib is likely not via inhibition of PARP activity.
In vivo
Patients received paclitaxel 175 mg/m(2) IV over 3h followed by carboplatin area under the curve (AUC)=six over 30 min on day one of 21 day cycles plus iniparib 4 mg/kg IV over 1h twice weekly beginning on day one. Iniparib plus paclitaxel and carboplatin did not show significant activity.
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