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Chemical Structure| 1426138-42-2 Chemical Structure| 1426138-42-2

Structure of FX1
CAS No.: 1426138-42-2

Chemical Structure| 1426138-42-2

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FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).

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Product Details of FX1

CAS No. :1426138-42-2
Formula : C14H9ClN2O4S2
M.W : 368.82
SMILES Code : O=C(O)CCN(C/1=O)C(SC1=C2C(NC3=C/2C=C(Cl)C=C3)=O)=S
MDL No. :MFCD31560474
InChI Key :JYBGCTWNOMSQJY-UHFFFAOYSA-N
Pubchem ID :135886621

Safety of FX1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02902679 Thrombosis Fa... More >>ctor XI Renal Impairment ESRD (End-Stage Renal Disease) Less << Phase 1 Completed - United States, Florida ... More >> Orlando Clinical Research Center Orlando, Florida, United States, 32809 Less <<
NCT00630864 Transthyretin-associated Amylo... More >>idosis With Polyneuropathy Less << Phase 2 Completed - United States, Maryland ... More >> Johns Hopkins Hospital Baltimore, Maryland, United States, 21205 France CHU de Bicetre Paris, France Germany Universitatsklinikum Munster, Transplant Hepatology Munster, Germany Italy Centro per lo Studio e la Cura delle Amiloidosi Sistemiche IRCCS - Policlinico San Matteo, Pavia, Italy, 19 - 27100 Less <<
NCT01358565 Mild Hepatic Dysfunction ... More >> Moderate Hepatic Dysfunction Less << Phase 1 Completed - South Africa ... More >> Pfizer Investigational Site Newton Park, Port Elizabeth, South Africa, 6045 Less <<
NCT00925002 ATTR-PN Phase 3 Active, not recruiting December 31, 2021 United States, Maryland ... More >> Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 Argentina FLENI Ciudad Autonoma de Buenos aires, Argentina, C1428AQK Brazil Hospital Universitário Clementino Fraga Filho -HUCFF Universidade Federal do Rio de Janeiro Rio de Janeiro, RJ, Brazil, CEP 21941-913 France CHU Henri Mondor Creteil cedex, France, 94010 Germany Universitatsklinikum Muenster Muenster, Germany, 48149 Italy Centro per lo Studio e la Cura delle Amiloidosi Sistemiche IRCCS - Policlinico San Matteo Pavia, Italy, 27100 Dipartimento di Neurofisiopatologia Pavia, Italy, 27100 Fondazione IRCCS Policlinico San Matteo Pavia, Italy, 27100 IRCCS Pavia, Italy, 27100 Portugal Centro Hospitalar Lisboa Norte, EPE- Hospital de Santa Maria Lisboa, Portugal, 1649-028 Unidade Clinica de Paramiloidose, EPE - Centro Hospitalar do Porto, Hospital Geral de Santo Antonio Porto, Portugal, 4099-001 Sweden Norrlands University Hospital Umea, Sweden, 90185 Umea Universtiy Hospital Umea, Sweden, 90187 Less <<
NCT00630864 - Completed - -
NCT00694161 - Completed - -
NCT00935012 TTR-CM Phase 3 Active, not recruiting December 2021 United States, Illinois ... More >> University of Chicago Medical Center Chicago, Illinois, United States, 60637 United States, Maryland Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 United States, Massachusetts Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 United States, New York Clinical Cardiovascular Research Lab for the Elderly (CCRLE) Columbia Universtiy New York, New York, United States, 10034 Less <<
NCT00694161 Cardiomyopathy Phase 2 Completed - United States, Georgia ... More >> Emory University School of Medicine Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Maryland Johns Hopkins Hospital Baltimore, Maryland, United States, 21205 United States, Massachusetts Harvard Vanguard Medical Associates Boston, Massachusetts, United States, 02215 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, New York Columbia University New York, New York, United States, 10032 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.56mL

2.71mL

1.36mL

27.11mL

5.42mL

2.71mL

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