A PARP1 inhibitor
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BSI-201

Item No. 11304

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-iodo-3-nitro-benzamide
CAS Number
160003-66-7
Synonyms
  • IND 71677
  • Iniparib
Molecular Formula
C7H5IN2O3
Formula Weight
292.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
242 nm
SMILES
NC(C1=CC([N+]([O-])=O)=C(I)C=C1)=O
InChi Code
InChI=1S/C7H5IN2O3/c8-5-2-1-4(7(9)11)3-6(5)10(12)13/h1-3H,(H2,9,11)
InChi Key
MDOJTZQKHMAPBK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $132

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    50 mg

    $395

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    100 mg

    $522

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    Cayman Chemical
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    Product Description

    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 BRCA2.1,2,3 BSI-201 is an irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain.1,2,4 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.5 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.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yuan, Y., Liao, Y.M., Hsueh, C.T., et al. Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011).

    2. Javle, M., and Curtin, N.J. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther. Adv. Med. Oncol. 3(6), 257-267 (2011).

    3. Plummer, R. Poly(ADP-ribose) polymerase inhibition: A new direction for BRCA and triple-negative breast cancer? Breast Cancer Res. 13(4), 1-6 (2011).

    4. Bauer, P.I., Mendeleyeva, J., Kirsten, E., et al. Anti-cancer action of 4-iodo-3-nitrobenzamide in combination with buthionine sulfoximine: Inactivation of poly(ADP-ribose) polymerase and tumor glycolysis and the appearance of a poly(ADP-ribose) polymerase protease. Biochem. Pharmacol. 63, 455-462 (2002).

    5. Mendeleyev, J., Kirsten, E., Hakam, A., et al. Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide. Biochem. Pharmacol. 50(5), 705-714 (1995).

    6. O'Shaughnessy, J., Osborne, C., Pippen, J.E., et al. Iniparib plus chemotherapy in metastatic triple-negative breast cancer. N. Engl. J. Med. 364(3), 205-214 (2011).