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编 号:F757668
分子式:C15H18N2O3S
分子量:306.38
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 μM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.

体内研究:
AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%.Animal Model:6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g
Dosage:2.5 mg/kg
Administration:intratumorally injected; week; 25 days
Result:Inhibited tumor growth and the final tumor growth inhibition is 65%.

体外研究:
AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 μM) shows excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM).AR antagonist 3 (0.01, 0.1, 1, 10, 100 μM) inhibits the proliferation of LNCaP cells.AR antagonist 3 (0.1, 1, 10 μM; 48 h) reduces the protein expression levels of c-Myc and KLK3.AR antagonist 3 (0.01, 0.1, 1, 10, 100 μM) exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM).AR antagonist 3 (10 μM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells.
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