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CAS No.: 1426138-42-2
Synonyms: FX1
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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生物活性
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NCT02902679 | Thrombosis Fa... more >>ctor XI Renal Impairment ESRD (End-Stage Renal Disease) Collapse << | Phase 1 | Completed | - | United States, Florida ... more >> Orlando Clinical Research Center Orlando, Florida, United States, 32809 Collapse << |
NCT00630864 | Transthyretin-associated Amylo... more >>idosis With Polyneuropathy Collapse << | 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 Collapse << |
NCT01358565 | Mild Hepatic Dysfunction ... more >> Moderate Hepatic Dysfunction Collapse << | Phase 1 | Completed | - | South Africa ... more >> Pfizer Investigational Site Newton Park, Port Elizabeth, South Africa, 6045 Collapse << |
实验方案
技术信息
CAS号 | 1426138-42-2 | 储存条件 |
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分子式 | C14H9ClN2O4S2 | 运输 | 蓝冰 | |||||||
分子量 | 368.82 | 别名 | FX1 | |||||||
溶解度 |
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动物实验配方 |