Identification | Back Directory | [Name]
BRD4-IN-1 FL-411 | [CAS]
2118944-88-8 | [Synonyms]
-411 FL-411 BRD4-IN-1 BRD4-IN-1 FL-411 FL-411;FL 411;FL411 Pyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(1H)-one, 5,6,7,8-tetrahydro-2-(4-hydroxy-3,5-dimethylphenyl)-7-methyl- | [Molecular Formula]
C18H19N3O2S | [MOL File]
2118944-88-8.mol | [Molecular Weight]
341.43 |
Chemical Properties | Back Directory | [Boiling point ]
577.5±60.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:5.4(Max Conc. mg/mL);15.82(Max Conc. mM) | [form ]
Solid | [pka]
8.97±0.40(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
FL 411, is a potent and selective BRD4 inhibitor. | [in vivo]
To evaluate the antitumor activity of FL-411 in vivo, two breast tumor xenograft models, namely, MCF-7 and MDA-MB-231 cell lines models, are used. The in vivo study is conducted using three different doses of FL-411: 25 mg/kg, 50 mg/kg, and 100 mg/kg. In all the models, FL-411 shows significant tumor growth inhibition in a dose-dependent manner as determined by 80% and 76% tumor growth inhibition ratio in MCF-7 and MDA-MB-231 cell models, respectively. A remarkable loss of tumor weights is observed in all dose groups (p<0.001). FL-411 displays no obvious effects on the body weight of all the treatment groups. To examine whether FL-411-mediated inhibition of tumor growth in vivo is associated with reduced cell proliferation and the increased autophagy-associated cell death, tumor tissues from control and FL-411-treated mice are processed for the immunohistochemical analysis of Ki-67 and LC3. FL-411 treatment obviously reduces the number of Ki-67 (p<0.001) positive cells as well as increases autophagy levels, which is determined by increased LC3 expression (p<0.001)[1]. | [IC 50]
BRD4(1): 0.43 μM (IC50) | [storage]
Store at -20°C |
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Company Name: |
Twochem Co.Ltd.
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Tel: |
021-58111628 15800915896 |
Website: |
cn.twochem.com |
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