Testing Data
Iniparib, Inhibitor
Iniparib (BSI-201)
Purity
0.998
Synonyms
Iniparib; Iniparib (BSI-201); inhibitor
Purity/Purification
0.998
Solubility
DMSO 58mg/mL - Water <1mg/mL - Ethanol 28mg/mL
Formula
C7H5IN2O3
Preparation and Storage
Store at-20 degree C 2 years.
Testing Data
Testing Data
Related Product Information for Iniparib, inhibitor
Description: BSI-201 is described as a prodrug of 4-iodo-3-nitrosobenzamide, an agent that covalently inhibits PARP1 by binding to its first zinc finger under cell-free conditions. Treatment of 120 muM BSI-201 plus buthionine sulfoximine (BSO) induces a 95% cell death among 855-2 cells, and displays a similar effect in other human cancer cells. BSI-201 inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. Recently BSI-201 shows no ability to inhibit PARP enzymatic or cellular activity, but can non-selectively modify cysteine-containing proteins in tumor cells, suggesting the mechanism of action for BSI-201 is likely not via inhibition of PARP activity. BSI-201 (100 muM) inhibits ionizing radiation-induced single-strand breaks (SSBs) repair in human lymphoid cell lines based on large endogenous Epstein-Barr virus (EBV) circular episomes assay, resulting in 55% repair by 2 hours, which can be reversed surprisingly by knockdown of PARP1, indicating that the mechanism of inhibition does not involve trapping PARP at SSBs. BSI-201 is not able to selectively kill homologous recombination (HR)-deficient cells between BRCA2-deficient PEO1 and BRCA2-revertant PEO4, or ATM-deficient GM16666 and ATM-restored GM16667 fibroblasts. BSI-201 is cytotoxic to a variety of cell lines at concentrations above 40 muM reflecting a mechanism independent of PARP.
Biological Activity: Iniparib (BSI-201) is a potent PARP1 inhibitor with strong anti-neoplastic effect. BSI-201 covalently binds and inhibits PARP-1. When given as a single agent and in combination with other cytotoxic agents, Iniparib (BSI-201) is active against a broad range of cancer cells in culture.Iniparib (BSI-201) has first-in-class and best-in-class potential as targeted therapy for several types of cancer. Iniparib (BSI-201) has demonstrated activity in multiple types of solid tumors, with prolonged inhibition of its target. Iniparib (BSI-201) has shown a strong safety profile. Iniparib (BSI-201) is a leading candidate in the field of PARP inhibitors and is the furthest along in clinical development of this novel therapeutic approach.
Biological Activity: Iniparib (BSI-201) is a potent PARP1 inhibitor with strong anti-neoplastic effect. BSI-201 covalently binds and inhibits PARP-1. When given as a single agent and in combination with other cytotoxic agents, Iniparib (BSI-201) is active against a broad range of cancer cells in culture.Iniparib (BSI-201) has first-in-class and best-in-class potential as targeted therapy for several types of cancer. Iniparib (BSI-201) has demonstrated activity in multiple types of solid tumors, with prolonged inhibition of its target. Iniparib (BSI-201) has shown a strong safety profile. Iniparib (BSI-201) is a leading candidate in the field of PARP inhibitors and is the furthest along in clinical development of this novel therapeutic approach.
Product Categories/Family for Iniparib, inhibitor
References
[1] Cancer Biology & Therapy 1 January 2009; 8:1, 2-3 [2] Acta Pharmacologica Sinica 2010; 31: 1172-1180; [3] Neuroscience 2010; 171:1256-1264 [4] Mendeleyev J, et al. Biochem Pharmacol, 1995, 50(5), 705-714. [5] Bauer PI, et al. Biochem Pharmacol, 2002, 63(3), 455-462. [6] Liu X, et al. Clin Cancer Res, 2012, 18(2), 510-523. [7] Ma W, et al. Proc Natl Acad Sci U S A, 2012, 109(17), 6590-6595. [8] Patel AG, et al. Clin Cancer Res, 2012, 18(6), 1655-1662. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
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Product Notes
The Iniparib (Catalog #AAA8506573) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Iniparib, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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