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BSI-201 New

Cayman Chemical Item Number 11304

Iniparib; IND 71677 (CAS 160003-66-7)

BSI-201 (CAS 160003-66-7)

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

1 Yuan, Y., Liao, Y., Hsueh, C., 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).

Synonyms
  • Iniparib
  • IND 71677
Formal Name 4-​iodo-​3-​nitro-​benzamide
CAS Number 160003-66-7
Molecular Formula C7H5IN2O3
Formula Weight 292.0
Formulation A crystalline solid
Purity ≥98%
λmax 242 nm
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
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NC(C1=CC([N+]​([O-]​)​=O)​=C(I)​C=C1)​=O
Size Price Quantity Subtotal
10 mg $98.00 $0.00
50 mg $295.00 $0.00
100 mg $389.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-26. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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