Research Area
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BSI-201 Chemical Structure
ABT-888 (Veliparib)
ABT-888 (Veliparib) is a potent poly (ADP-ribose) polymerase (PARP) inhibitor of PARP-1 and PARP-2 with Ki of 5.2 nM and 2.9 nM, respectively.
Olaparib (AZD2281)
Olaparib(AZD2281, KU0059436) is a selective inhibitor of PARP-1 and PARP-2 enzymes with IC50 of 5 nM and 1 nM, respectively.
Rucaparib (AG-014699 , PF-01367338)
AG-014699 (Rucaparib, PF-01367338) is an inhibitor of PARP with a Ki of 1.4 nM.
INO-1001
INO-1001 is a novel potent PARP inhibitor with an IC50 of 3 nM.
AG14361
AG14361 is a potent inhibitor of purified full-length human PARP-1 with Ki of less than 5 nM.
MK-4827
MK-4827 is a potent, selective PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively.
Pemetrexed (Alimta)
Pemetrexed (Alimta) is a thymidylate synthase, DHFR and glycinamide ribonucleotide formyltransferase inhibitor with an IC50 of 25, 34, 220 nM.
Bleomycin sulfate
A glycopeptide antibiotic produced by the bacterium Streptomyces verticillus.
Clofarabine
Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase
Biological Activity
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, BSI-201 is active against a broad range of cancer cells in culture. BSI-201 has first-in-class and best-in-class potential as targeted therapy for several types of cancer. BSI-201 has demonstrated activity in multiple types of solid tumors, with prolonged inhibition of its target. BSI-201 has shown a strong safety profile. 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. [1][2][3]
References on BSI-201
- [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
Product Information
| Molecular Weight (WM): | 292.03 |
|---|---|
| Formula: | C7H5IN2O3 |
| CAS No.: | 160003-66-7 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥58mg/mL |
| Water <1mg/mL | |
| Ethanol ≥37mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
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Selleck's high quality products have been used in several published research findings, including the following:
Tumor necrosis factor-like weak inducer of apoptosis and fibroblast growth factor-inducible 14 mediate cerebral ischemia-induced poly(ADP-ribose) polymerase-1 activation and neuronal death.
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Representative Western blot analysis and quantification of the mean intensity of the band of IKB phosphorylation (E) and caspase 3 activation (F) in Wt neurons incubated with TWEAK either alone or in combination with the PARP-1 inhibitor BSI-201.
Representative Western blot analysis and quantification of the mean intensity of the band of IKB phosphorylation (E) and caspase 3 activation (F) in Wt neurons incubated with TWEAK either alone or in combination with the PARP-1 inhibitor BSI-201.
Data from [Neuroscience 2010.October;171:1256–1264] BSI-201 purchased from Selleck
- It has worked very well.
Asst Prof. Joseph A. De SotoLaboratory of Translational Oncology Department of Health, Injury, and Disease Management Uniformed Services University of the Health Sciences
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Representative Western blot analysis and quantification of the mean intensity of the band of IKB phosphorylation (E) and caspase 3 activation (F) in Wt neurons incubated with TWEAK either alone or in combination with the PARP-1 inhibitor BSI-201.
|
Data from [Neuroscience 2010.October;171:1256–1264]
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