{"id":"https://openalex.org/W2090769726","doi":"https://doi.org/10.1158/1538-7445.am2012-3783","title":"Abstract 3783: Pharmacokinetics and CNS biodistribution of WP1066, a novel small molecule inhibitor of STAT-3 phosphorylation","display_name":"Abstract 3783: Pharmacokinetics and CNS biodistribution of WP1066, a novel small molecule inhibitor of STAT-3 phosphorylation","publication_year":2012,"publication_date":"2012-04-01","ids":{"openalex":"https://openalex.org/W2090769726","doi":"https://doi.org/10.1158/1538-7445.am2012-3783","mag":"2090769726"},"language":"en","primary_location":{"id":"doi:10.1158/1538-7445.am2012-3783","doi":"https://doi.org/10.1158/1538-7445.am2012-3783","is_oa":false,"landing_page_url":"https://doi.org/10.1158/1538-7445.am2012-3783","pdf_url":null,"source":{"id":"https://openalex.org/S168522863","display_name":"Cancer Research","issn_l":"0008-5472","issn":["0008-5472","1538-7445"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","doyens","jufo-3","ki-jl-3","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320273","host_organization_name":"American Association for Cancer Research","host_organization_lineage":["https://openalex.org/P4310320273"],"host_organization_lineage_names":["American Association for Cancer Research"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Cancer Research","raw_type":"journal-article"},"volume":null,"type":"conference-abstract","indexed_in":["crossref"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5086839893","display_name":"Timothy L. Madden","orcid":"https://orcid.org/0000-0003-2954-4776","observed_orcids":["https://orcid.org/0000-0003-2954-4776"]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Timothy Madden","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5016121227","display_name":"Mary J. Johansen","orcid":"https://orcid.org/0000-0003-0118-2224","observed_orcids":["https://orcid.org/0000-0003-0118-2224"]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Mary Johansen","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5049265932","display_name":"Kirk Salvatore Culotta","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Kirk S. Culotta","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079081497","display_name":"Amy B. Heimberger","orcid":"https://orcid.org/0000-0002-9970-8695","observed_orcids":["https://orcid.org/0000-0002-9970-8695"]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Amy Heimberger","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5055645760","display_name":"Izabela Fokt","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Izabela Fokt","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5106083527","display_name":"Charles A. Conrad","orcid":"https://orcid.org/0000-0001-5178-8465","observed_orcids":["https://orcid.org/0000-0001-5178-8465"]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Charles Conrad","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5062959791","display_name":"Waldemar Priebe","orcid":"https://orcid.org/0000-0003-4522-4772","observed_orcids":["https://orcid.org/0000-0003-4522-4772","https://orcid.org/0000-0003-3969-0144"]},"institutions":[{"id":"https://openalex.org/I1343551460","display_name":"The University of Texas MD Anderson Cancer Center","ror":"https://ror.org/04twxam07","country_code":"US","type":"healthcare","lineage":["https://openalex.org/I1343551460"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Waldemar Priebe","raw_affiliation_strings":["1UT MD Anderson Cancer Ctr., Houston, TX"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1UT MD Anderson Cancer Ctr., Houston, TX","institution_ids":["https://openalex.org/I1343551460"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":["https://openalex.org/I1343551460"],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":"72","issue":"8_Supplement","first_page":"3783","last_page":"3783"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11503","display_name":"Cytokine Signaling Pathways and Interactions","score":0.9359999895095825,"subfield":{"id":"https://openalex.org/subfields/2730","display_name":"Oncology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T11503","display_name":"Cytokine Signaling Pathways and Interactions","score":0.9359999895095825,"subfield":{"id":"https://openalex.org/subfields/2730","display_name":"Oncology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10129","display_name":"Glioma Diagnosis and Treatment","score":0.04100000113248825,"subfield":{"id":"https://openalex.org/subfields/2716","display_name":"Genetics (clinical)"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.0027000000700354576,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/wp1066","display_name":"WP1066","score":0.9869999885559082},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.9160000085830688},{"id":"https://openalex.org/keywords/brain-penetration","display_name":"brain penetration","score":0.6909999847412109},{"id":"https://openalex.org/keywords/oral-bioavailability","display_name":"oral bioavailability","score":0.5460000038146973},{"id":"https://openalex.org/keywords/high-grade-glioma","display_name":"high-grade glioma","score":0.7599999904632568},{"id":"https://openalex.org/keywords/glioblastoma","display_name":"glioblastoma","score":0.6330000162124634},{"id":"https://openalex.org/keywords/apoptosis","display_name":"apoptosis","score":0.38999998569488525},{"id":"https://openalex.org/keywords/c-myc","display_name":"c-Myc","score":0.7440000176429749},{"id":"https://openalex.org/keywords/bcl-xl","display_name":"Bcl-xL","score":0.9670000076293945},{"id":"https://openalex.org/keywords/mcl-1","display_name":"Mcl-1","score":0.9950000047683716},{"id":"https://openalex.org/keywords/xenografts","display_name":"xenografts","score":0.6259999871253967},{"id":"https://openalex.org/keywords/lc-ms-ms-quantification","display_name":"LC-MS/MS quantification","score":0.8289999961853027},{"id":"https://openalex.org/keywords/non-compartmental-analysis","display_name":"non-compartmental analysis","score":0.7950000166893005},{"id":"https://openalex.org/keywords/dosing-regimen","display_name":"dosing regimen","score":0.7300000190734863},{"id":"https://openalex.org/keywords/mouse-model","display_name":"mouse model","score":0.3319999873638153},{"id":"https://openalex.org/keywords/plasma-protein-binding","display_name":"plasma protein binding","score":0.34599998593330383}],"concepts":[{"id":"https://openalex.org/C2777807558","wikidata":"https://www.wikidata.org/wiki/Q4914764","display_name":"Biodistribution","level":3,"score":0.8098397254943848},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.7816814184188843},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.6547483205795288},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.6540569067001343},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.5190035104751587},{"id":"https://openalex.org/C2777288759","wikidata":"https://www.wikidata.org/wiki/Q4164182","display_name":"Dosing","level":2,"score":0.48728787899017334},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.3656216859817505},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.20028379559516907},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1158/1538-7445.am2012-3783","doi":"https://doi.org/10.1158/1538-7445.am2012-3783","is_oa":false,"landing_page_url":"https://doi.org/10.1158/1538-7445.am2012-3783","pdf_url":null,"source":{"id":"https://openalex.org/S168522863","display_name":"Cancer Research","issn_l":"0008-5472","issn":["0008-5472","1538-7445"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","doyens","jufo-3","ki-jl-3","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320273","host_organization_name":"American Association for Cancer Research","host_organization_lineage":["https://openalex.org/P4310320273"],"host_organization_lineage_names":["American Association for Cancer Research"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Cancer Research","raw_type":"journal-article"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.9391000270843506,"id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W1576752489","https://openalex.org/W2151513527","https://openalex.org/W1971358650","https://openalex.org/W2506649274","https://openalex.org/W2033091977","https://openalex.org/W3206759263","https://openalex.org/W1590504688","https://openalex.org/W7099653178","https://openalex.org/W2153978030","https://openalex.org/W2062360007"],"abstract_inverted_index":{"Abstract":[0],"Utilizing":[1],"molecular":[2],"modeling":[3],"and":[4,10,32,34,57,90,143,186,198,233,248,254,273,299,308,331,340,419],"medicinal":[5],"chemistry":[6],"we":[7,73,103],"have":[8],"designed":[9,74],"discovered":[11],"novel,":[12],"potent":[13],"small":[14],"molecule":[15],"inhibitors":[16],"of":[17,40,53,60,77,85,100,109,120,122,162,193,207,212,265,303,407,417,423,438,443],"STAT3":[18],"activation.":[19],"WP1066,":[20],"our":[21],"lead":[22],"compound,":[23],"suppressed":[24],"several":[25],"downstream":[26],"signaling":[27],"products":[28],"including":[29],"c-myc,":[30],"Bcl-XL":[31],"Mcl-1,":[33],"induced":[35],"apoptosis":[36],"in":[37,49,78,93,209,223,250,390,392,409,427],"a":[38,75,94,118,159,210,316,354,404,414],"panel":[39],"malignant":[41,54],"gliomas.":[42],"Further":[43],"studies":[44,80],"demonstrated":[45],"that":[46,385],"WP1066":[47,72,111,165,281,375],"inhibited,":[48],"vivo,":[50],"the":[51,67,83,98,134,147,262,421,439,444],"growth":[52],"glioma":[55],"xenografts":[56],"decreased":[58],"levels":[59],"phosphorylated":[61],"STAT3.":[62],"In":[63],"order":[64],"to":[65,81,133,146,277,294,366,387],"determine":[66],"best":[68],"dosing":[69,370,426],"schedule":[70],"for":[71,403,447],"number":[76],"vivo":[79],"assess":[82],"biodistribution":[84],"this":[86,101,410],"agent":[87],"following":[88,315,324,413],"oral":[89,148,325],"intravenous":[91,135],"administration":[92,161,326],"mouse":[95,157,411],"model.":[96],"For":[97],"purposes":[99],"study":[102,373],"developed":[104],"LC/MS/MS":[105],"analytical":[106],"methods":[107],"capable":[108],"quantifying":[110],"extracted":[112],"from":[113,191,241,292],"plasma":[114,228,300,332],"or":[115,125,166,171],"tissues":[116],"having":[117],"limit":[119],"quantification":[121],"1":[123],"ng/ml":[124],"gm":[126],"tissue.":[127],"80":[128],"female":[129],"mice":[130,145],"were":[131,175,221,275,401],"assigned":[132],"arm":[136,149],"(16":[137],"timepoints,":[138,151],"5":[139,152,213,266],"animals":[140,153,194,214,243],"per":[141,154],"timepoint)":[142],"65":[144],"(13":[150],"timepoint).":[155],"Each":[156],"received":[158],"single":[160,415],"40":[163,317],"mg/kg":[164,318],"control":[167,216],"vehicle,":[168],"either":[169],"orally":[170],"intravenously.":[172],"Blood":[173,197,219],"samples":[174,220,268],"collected":[176,190,203,222],"by":[177,231],"cardiac":[178],"puncture":[179],"under":[180],"isoflurane":[181],"anesthesia.":[182],"At":[183],"sacrifice":[184],"blood":[185],"brain":[187,199],"tissue":[188,200,240,330],"was":[189,201,229,244,327,348],"groups":[192],"receiving":[195,215],"WP1066.":[196],"also":[202],"within":[204],"30":[205],"minutes":[206],"injection":[208],"group":[211],"vehicle":[217],"alone.":[218],"appropriately":[224,251],"labeled":[225,252],"heparinized":[226],"tubes,":[227],"generated":[230],"centrifugation":[232],"frozen":[234,255],"at":[235,256,269,358,379],"\u201380\u00b0C":[236,257],"until":[237,258],"analyzed.":[238,259],"Brain":[239],"all":[242],"harvested,":[245],"blotted,":[246],"weighed,":[247],"placed":[249],"cryotubes":[253],"Following":[260],"analysis":[261],"mean":[263,297,355],"value":[264],"measured":[267],"each":[270],"timepoint":[271],"(plasma":[272],"brain)":[274],"subject":[276],"non-compartmental":[278],"PK":[279],"analysis.":[280],"showed":[282],"excellent":[283],"CNS":[284,298,322,377],"bioavailability":[285,347],"with":[286,329,362],"concurrent":[287],"brain-to-blood":[288],"concentration":[289,357],"ratios":[290],"ranging":[291],"10:1":[293],"100:1,":[295],"reaching":[296,335,353],"peak":[301,333,356],"concentrations":[302,334,364,378,383,400],"57.6":[304],"\u00b5g/g":[305,337],"(162.2":[306],"\u03bcM)":[307,339],"0.6":[309],"\u00b5g":[310],"/mL":[311],"(1.8":[312],"\u03bcM),":[313,344],"respectively,":[314],"IV":[319],"bolus":[320],"administration.":[321,371],"penetration":[323],"similar":[328],"2.7":[336],"(7.6":[338],"0.09":[341],"\u00b5g/mL":[342],"(0.3":[343],"respectively.":[345],"Oral":[346],"36.3%":[349],"(AUC":[350],"PO/AUC":[351],"IV),":[352],"0.75":[359],"hours":[360,368],"postdose":[361],"measureable":[363],"up":[365],"8":[367],"after":[369],"This":[372],"demonstrates":[374],"maintains":[376],"many":[380,393],"fold":[381],"higher":[382],"than":[384],"needed":[386],"demonstrate":[388],"activity":[389],"vitro":[391],"cancer":[394],"cell":[395],"lines":[396],"(1":[397],"\u00b5M).":[398],"These":[399],"maintained":[402],"significant":[405],"period":[406],"time":[408],"model":[412],"dose":[416],"drug,":[418],"support":[420],"use":[422],"once":[424],"daily":[425],"clinical":[428],"trials.":[429],"Citation":[430],"Format:":[431],"{Authors}.":[432],"{Abstract":[433],"title}":[434],"[abstract].":[435],"In:":[436],"Proceedings":[437],"103rd":[440],"Annual":[441],"Meeting":[442],"American":[445],"Association":[446],"Cancer":[448,459],"Research;":[449],"2012":[450],"Mar":[451],"31-Apr":[452],"4;":[453],"Chicago,":[454],"IL.":[455],"Philadelphia":[456],"(PA):":[457],"AACR;":[458],"Res":[460],"2012;72(8":[461],"Suppl):Abstract":[462],"nr":[463],"3783.":[464],"doi:1538-7445.AM2012-3783":[465]},"counts_by_year":[],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}
