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编 号：F754707
分子式：C21H24FN5
分子量：365.45
分子式：C21H24FN5
分子量：365.45
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CAS No: 2698340-11-1
产品详情
生物活性：
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
体内研究：
LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability.Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats.IV (2 mg/kg)IG (10 mg/kg)
C0 (ng/mL)575Cmax (ng/mL)41.1
T1/2 (h)1.0T1/2 (h)2.8
Vdss (L/kg)6.6Tmax (h)0.8
Cl (mL/min/kg)156AUC0-t (ng.h/mL)126
AUC0-t (ng.h/mL)211AUC0-∞ (ng.h/mL)152
AUC0-∞ (ng.h/mL)214Bioacailability (%)11.9
Animal Model:Male Sprague-Dawley rats
Dosage:2 mg/kg for i.v., 10 mg/kg for i.g.
Administration:i.v. and i.g, single
Result:Showed an acceptable half-life and oral bioavailability.
体外研究：
LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner.LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg.
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
体内研究：
LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability.Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats.IV (2 mg/kg)IG (10 mg/kg)
C0 (ng/mL)575Cmax (ng/mL)41.1
T1/2 (h)1.0T1/2 (h)2.8
Vdss (L/kg)6.6Tmax (h)0.8
Cl (mL/min/kg)156AUC0-t (ng.h/mL)126
AUC0-t (ng.h/mL)211AUC0-∞ (ng.h/mL)152
AUC0-∞ (ng.h/mL)214Bioacailability (%)11.9
Animal Model:Male Sprague-Dawley rats
Dosage:2 mg/kg for i.v., 10 mg/kg for i.g.
Administration:i.v. and i.g, single
Result:Showed an acceptable half-life and oral bioavailability.
体外研究：
LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner.LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg.
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