|3-硝基-4-碘苯甲酰胺|CsnPharm

CAS No.: 160003-66-7

Iniparib/3-硝基-4-碘苯甲酰胺 Catalog No. CSN12304

Synonyms: BSI-201;NSC-746045;IND-71677

BSI-201 is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC).

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实验方案

技术信息

生物活性

描述PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. BSI-201 is a unique PARP1 inhibitor for its little inhibitory potency on PARP enzymatic activity. However, it can target the zinc finger domain and prevents PARP-1 activation by DNA breaks, as well as non-selectively modifies cysteine-containing proteins in tumor cells^[1]^[2]. The addition of DL-buthionine sulfoximine to BSI-201 produced a more significant effect on proliferation in MDA-MB-231 and MDA-MB-436 cells, whereas BSI-201 alone had little effect^[2]. A phase II trial of BSI-201 combined with gemcitabine and carboplatin for the treatment of TN breast cancer have been done^[3].
作用机制BSI-201 targets the zinc finger domain and prevents PARP-1 activation by DNA breaks.^[1]
动物研究
剂量
Hamster: 200 mg/kg^[1] (i.p.)

给药途径
i.p.
临床研究

动物研究
剂量	Hamster: 200 mg/kg^[1] (i.p.)
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01593228	Solid Tumors	Phase 3	Completed	-	-
NCT01455532	Neoplasm Malignant	Phase 1	Completed	-	United States, Arizona ... more >> Investigational Site Number 840002 Scottsdale, Arizona, United States, 85258 United States, California Investigational Site Number 840004 Los Angeles, California, United States, 90048 United States, Georgia Investigational Site Number 840010 Augusta, Georgia, United States, 30912 United States, Missouri Investigational Site Number 840007 St Louis, Missouri, United States, 63110 United States, Ohio Investigational Site Number 840001 Cincinnati, Ohio, United States, 45267-0542 United States, Texas Investigational Site Number 840006 San Antonio, Texas, United States, 78229 Collapse <<
NCT00813956	Triple Negative Breast Cancer	Phase 2	Completed	-	United States, California ... more >> Stanford Comprehensive Cancer Center Stanford, California, United States, 94305 United States, Pennsylvania PrECOG Philadelphia, Pennsylvania, United States, 19103 Collapse <<

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参考文献

[1] Mendeleyev J, Kirsten E, et al. Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide. Metabolic reduction to the 3-nitroso derivative and induction of cell death in tumor cells in culture. Biochem Pharmacol. 1995 Aug 25;50(5):705-14.
[2] Liu X, Shi Y, et al. Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res. 2012 Jan 15;18(2):510-23.
[3] O'Shaughnessy J, Osborne C, et al. Iniparib plus chemotherapy in metastatic triple-negative breast cancer. N Engl J Med. 2011 Jan 20;364(3):205-14.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4243 mL
- 17.1215 mL
- 34.2430 mL
- 5 mM
- 0.6849 mL
- 3.4243 mL
- 6.8486 mL
- 10 mM
- 0.3424 mL
- 1.7121 mL
- 3.4243 mL

技术信息

CAS号

160003-66-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C7H5IN2O3

运输

蓝冰

分子量

292.03

别名

BSI-201;NSC-746045;IND-71677;ND-71677;NIBA;INO-2BA;SAR-240550

溶解度

DMSO	58.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	27.0 mg/mL (92.5 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01593228	Solid Tumors	Phase 3	Completed	-	-
NCT01455532	Neoplasm Malignant	Phase 1	Completed	-	United States, Arizona ... more >> Investigational Site Number 840002 Scottsdale, Arizona, United States, 85258 United States, California Investigational Site Number 840004 Los Angeles, California, United States, 90048 United States, Georgia Investigational Site Number 840010 Augusta, Georgia, United States, 30912 United States, Missouri Investigational Site Number 840007 St Louis, Missouri, United States, 63110 United States, Ohio Investigational Site Number 840001 Cincinnati, Ohio, United States, 45267-0542 United States, Texas Investigational Site Number 840006 San Antonio, Texas, United States, 78229 Collapse <<
NCT00813956	Triple Negative Breast Cancer	Phase 2	Completed	-	United States, California ... more >> Stanford Comprehensive Cancer Center Stanford, California, United States, 94305 United States, Pennsylvania PrECOG Philadelphia, Pennsylvania, United States, 19103 Collapse <<
NCT01204125	Breast Cancer Female	Phase 2	Completed	-	France ... more >> Investigational Site Number 250001 Besancon Cedex, France, 25030 Investigational Site Number 250004 Bordeaux, France, 33076 Investigational Site Number 250006 Bron Cedex, France, 69677 Investigational Site Number 250003 Paris Cedex 10, France, 75475 Investigational Site Number 250002 Toulouse, France, 31052 Investigational Site Number 250005 Villejuif, France, 94805 Germany Investigational Site Number 276003 Erlangen, Germany, 91054 Investigational Site Number 276004 Hamburg, Germany, 20357 Investigational Site Number 276002 Köln, Germany, 50931 Investigational Site Number 276001 Mönchengladbach, Germany, 41061 Spain Investigational Site Number 724001 Barcelona, Spain, 08035 Investigational Site Number 724009 Cáceres, Spain, 10003 Investigational Site Number 724013 Córdoba, Spain, 14004 Investigational Site Number 724006 Islas Baleares, Spain, 07014 Investigational Site Number 724012 Jaén, Spain, 23007 Investigational Site Number 724002 Lérida, Spain, 25198 Investigational Site Number 724005 Madrid, Spain, 28033 Investigational Site Number 724016 Madrid, Spain, 28041 Investigational Site Number 724007 Reus, Spain, 43201 Investigational Site Number 724018 Santiago De Compostela, Spain, 15706 Investigational Site Number 724017 Sevilla, Spain, 41009 Investigational Site Number 724010 Sevilla, Spain, 41013 Investigational Site Number 724003 Torrevieja, Spain, 03186 Investigational Site Number 724011 Valencia, Spain, 46009 Investigational Site Number 724015 Valencia, Spain, 46010 Collapse <<
NCT01173497	Estrogen Receptor Negative (ER... more >>-Negative) Breast Cancer Progesterone Receptor Negative (PR-Negative) Breast Cancer Human Epidermal Growth Factor Receptor 2 Negative (HER2-Negative) Breast Cancer Brain Metastases Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> University of Alabama At Birmingham Birmingham, Alabama, United States United States, California University of California At San Francisco San Francisco, California, United States United States, District of Columbia Georgetown University Washington, District of Columbia, United States United States, Illinois University of Chicago Chicago, Illinois, United States United States, Indiana Indiana University Simon Cancer Center Indianapolis, Indiana, United States United States, Maryland Johns Hopkins University Baltimore, Maryland, United States United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States United States, Michigan University of Michigan Ann Arbor, Michigan, United States United States, North Carolina University of North Carolina-CH Lineberger Comprehensive Cancer Center Chapel Hill, North Carolina, United States, 27599-7295 Duke University Durham, North Carolina, United States United States, Pennsylvania University of Pittsburgh Medical Center Pittsburgh, Pennsylvania, United States United States, Tennessee Vanderbilt University Nashville, Tennessee, United States United States, Texas MD Anderson Cancer Center Houston, Texas, United States Collapse <<
NCT01213381	Advance Solid Tumors	Phase 1	Completed	-	Japan ... more >> Sanofi-Aventis Investigational Site Number 392001 Kobe-Shi, Japan Sanofi-Aventis Investigational Site Number 392002 Matsuyama-Shi, Japan Collapse <<
NCT00422682	Tumors	Phase 1	Completed	-	United States, Connecticut ... more >> Research Site New Haven, Connecticut, United States United States, Michigan Research Site Detroit, Michigan, United States United States, New York Research Site New York City, New York, United States United States, Pennsylvania Research Site Philadelphia, Pennsylvania, United States United States, Texas Research Site Houston, Texas, United States Research Site San Antonio, Texas, United States Collapse <<
NCT01130259	-	-	-	-	-
NCT01086254	Non-small Cell Lung Cancer Sta... more >>ge IV Collapse <<	Phase 2	Completed	-	France ... more >> Sanofi-Aventis Investigational Site Number 250002 Caen Cedex, France, 14033 Sanofi-Aventis Investigational Site Number 250003 Marseille Cedex 09, France, 13009 Sanofi-Aventis Investigational Site Number 250004 Toulouse, France, 31059 Sanofi-Aventis Investigational Site Number 250001 Villejuif, France, 94805 Germany Sanofi-Aventis Investigational Site Number 276003 Essen, Germany, 45122 Sanofi-Aventis Investigational Site Number 276002 Gauting, Germany, 82131 Sanofi-Aventis Investigational Site Number 276001 Großhansdorf, Germany, 22927 Italy Sanofi-Aventis Investigational Site Number 380003 Livorno, Italy, 57123 Sanofi-Aventis Investigational Site Number 380001 Orbassano, Italy, 10043 Sanofi-Aventis Investigational Site Number 380002 Rozzano, Italy, 20089 Spain Sanofi-Aventis Investigational Site Number 724001 Badalona, Spain, 08916 Sanofi-Aventis Investigational Site Number 724002 Barcelona, Spain, 08035 United Kingdom Sanofi-Aventis Investigational Site Number 826001 Newcastle Upon Tyne, United Kingdom, NE7 7DN Sanofi-Aventis Investigational Site Number 826002 Wolverhampton, United Kingdom, WV10 0QP Collapse <<
NCT00540358	Breast Cancer	Phase 2	Completed	-	United States, Alabama ... more >> Research Site Birmingham, Alabama, United States United States, Colorado Research Site Denver, Colorado, United States United States, Connecticut Research Site Torrington, Connecticut, United States United States, Florida Research Site Ocoee, Florida, United States United States, Indiana Research Site Indianapolis, Indiana, United States United States, Kansas Research Site Overland Park, Kansas, United States United States, Nevada Research Site Henderson, Nevada, United States United States, New Hampshire Research Site Hooksett, New Hampshire, United States United States, North Carolina Research Site Raleigh, North Carolina, United States United States, Texas Research Site Bedford, Texas, United States Research Site Dallas, Texas, United States Research Site El Paso, Texas, United States Research Site Fort Worth, Texas, United States Research Site Houston, Texas, United States Research Site Tyler, Texas, United States United States, Virginia Research Site Fairfax, Virginia, United States United States, Washington Research Site Vancouver, Washington, United States Research Site Yakima, Washington, United States Collapse <<
NCT00938652	Breast Cancer	Phase 3	Completed	-	-
NCT00298675	Tumors	Phase 1	Completed	-	United States, Connecticut ... more >> Research Site New Haven, Connecticut, United States United States, Texas Research Site Houston, Texas, United States Research Site San Antonio, Texas, United States Collapse <<
NCT01045304	Breast Cancer, Metastatic	Phase 2	Completed	-	Australia ... more >> Sanofi-Aventis Investigational Site Number 036002 Parkville, Australia, 3052 Sanofi-Aventis Investigational Site Number 036001 Perth, Australia, 6000 Sanofi-Aventis Investigational Site Number 036003 Westmead, Australia, 2145 Belgium Sanofi-Aventis Investigational Site Number 056001 Bruxelles, Belgium, 1000 Sanofi-Aventis Investigational Site Number 056002 Leuven, Belgium, 3000 France Sanofi-Aventis Investigational Site Number 250005 Besancon Cedex, France, 25030 Sanofi-Aventis Investigational Site Number 250003 Bordeaux, France, 33076 Sanofi-Aventis Investigational Site Number 250002 Dijon, France, 21034 Sanofi-Aventis Investigational Site Number 250006 Paris Cedex 05, France, 75231 Sanofi-Aventis Investigational Site Number 250004 Paris, France, 75970 Sanofi-Aventis Investigational Site Number 250001 Toulouse, France, 31052 Italy Sanofi-Aventis Investigational Site Number 380004 Genova, Italy, 16132 Sanofi-Aventis Investigational Site Number 380001 Milano, Italy, 20133 Sanofi-Aventis Investigational Site Number 380002 Modena, Italy, 41100 Sanofi-Aventis Investigational Site Number 380003 Udine, Italy, 33100 Netherlands Sanofi-Aventis Investigational Site Number 528001 Rotterdam, Netherlands, 3075 EA Spain Sanofi-Aventis Investigational Site Number 724002 Barcelona, Spain, 08035 Sanofi-Aventis Investigational Site Number 724004 Madrid, Spain, 28050 Sanofi-Aventis Investigational Site Number 724001 Málaga, Spain, 29010 Sanofi-Aventis Investigational Site Number 724003 Valencia, Spain, 46010 Collapse <<
NCT01082549	Squamous Cell Lung Cancer	Phase 3	Completed	-	-
NCT00677079	Primary Peritoneal Cancer ... more >> Advanced Epithelial Ovarian Cancer Collapse <<	Phase 2	Completed	-	United States, New York ... more >> New York, New York, United States, 10021 Collapse <<
NCT00687765	Glioblastoma	Phase 1 Phase 2	Completed	-	United States, Alabama ... more >> Research Site Birmingham, Alabama, United States, 35294 United States, Florida Research Site Tampa, Florida, United States, 33612 United States, Georgia Research Site Atlanta, Georgia, United States, 30322 United States, Maryland Research Site Baltimore, Maryland, United States United States, Massachusetts Research Site Boston, Massachusetts, United States, 92114 United States, Michigan Research Site Detroit, Michigan, United States, 48202 United States, North Carolina Research Site Winston Salem, North Carolina, United States, 27157 United States, Pennsylvania Research Site Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT01161836	Advanced Solid Tumors	Phase 1	Completed	-	United States, Washington ... more >> Northwest Medical Specialties Tacoma, Washington, United States, 98405 Collapse <<
NCT01033123	Ovarian Cancer	Phase 2	Completed	-	United States, Massachusetts ... more >> Massachusetts Ceneral Hospital Boston, Massachusetts, United States, 02114 Collapse <<
NCT01551680	Brain Metastases	Phase 1	Terminated(end of study of thi... more >>s product) Collapse <<	-	France ... more >> CRLC Val d'Aurelle-Paul Lamarque Montpellier, France, 34298 AP-HP Hôpital Saint-Louis Paris, France Institut Gustave-Roussy Villejuif, France Collapse <<
NCT01033292	Ovarian Cancer	Phase 2	Completed	-	United States, Massachusetts ... more >> Massachusetts Ceneral Hospital Boston, Massachusetts, United States, 02114 Collapse <<
NCT00687687	Uterine Carcinosarcoma	Phase 2	Completed	-	-

Iniparib/3-硝基-4-碘苯甲酰胺 Catalog No. CSN12304

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