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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 50 mg/mL|
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.
|Related PARP Products|
|Niraparib (MK-4827) tosylate
Niraparib (MK-4827) tosylate is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.
Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
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