Iniparib (BSI-201) , ≥98% , 160003-66-7
Synonym(s):
4-Iodo-3-nitrobenzamide;BSI-201
CAS NO.：160003-66-7
Empirical Formula: C7H5IN2O3
Molecular Weight: 292.03
MDL number: MFCD11110639
EINECS: 685-396-9
| Pack Size | Price | Stock | Quantity |
| 10MG | RMB23.20 | In Stock |
|
| 50MG | RMB39.20 | In Stock |
|
| 250MG | RMB69.60 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 150-153° |
| Boiling point: | 344.8±32.0 °C(Predicted) |
| Density | 2.055±0.06 g/cm3(Predicted) |
| storage temp. | Sealed in dry,Store in freezer, under -20°C |
| solubility | DMSO: soluble5mg/mL, clear |
| form | powder |
| pka | 14+-.0.50(Predicted) |
| color | white to beige |
| Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| InChI | 1S/C7H5IN2O3/c8-5-2-1-4(7(9)11)3-6(5)10(12)13/h1-3H,(H2,9,11) |
| InChIKey | MDOJTZQKHMAPBK-UHFFFAOYSA-N |
| SMILES | NC(C1=CC=C(C([N+]([O-])=O)=C1)I)=O |
Description and Uses
Iniparib (160003-66-7) was originally thought to be a PARP1 inhibitor but this is controversial.1,2Inhibits ionizing radiation-induced single-stranded DNA break repair in lymphoid cell linesin vivo.3Inhibits growth of certain breast cancer cell linesin vitro. Iniparib non-selectively modifies cysteine-containing proteins in tumor cells.4
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. Inhibiting its activity has been linked to synthetic lethality and loss of either of the breast cancer susceptibility genes, BRCA1 and BRCA2. BSI-201 is an irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain. It 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. In phase II clinical studies, BSI-201, in combination with carboplatin and gemcitabine, has produced promising results in "triple-negative" breast cancers, increasing median overall survival from 7.7 months to 12.3 months.
