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Iniparib

Cat. No. M1972
Iniparib Structure
Synonym:

BSI-201, NSC-746045, IND-71677

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 292.03
Formula C7H5IN2O3
CAS Number 160003-66-7
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

Differential effects of poly(ADP-ribose) polymerase inhibition on DNA break repair in human cells are revealed with Epstein-Barr virus.
Ma W, et al. Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6590-5. PMID: 22493268.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Iniparib, BSI-201, NSC-746045, IND-71677 supplier, PARP, inhibitors

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