产品
编 号：F753321
分子式：C17H16F4N2O4S
分子量：420.38
分子式：C17H16F4N2O4S
分子量：420.38
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CAS No: 2490284-25-6
产品详情
生物活性：
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
体内研究：
NN-390 (male CD-1 mice, 20 mg/kg, IP, single dose) increases plasma stability.NN-390 can improve PAMPA (parallel artificial membrane permeability assay)-BBB (blood-brain barrier) score.Pharmacokinetic Parameters of NN-390 in male male CD-1 mice.CompoundKT-531 5a; NN-390
t1/2 (h)1.051.90
Cmax (ng/mL)493750
AUClast (h*ng/mL)15762523
AUClnf (h*ng/mL)15192548
AUC/D (h*ng/mL)79126
Animal Model:CD-1 mice (male, n=3)
Dosage:20 mg/kg
Administration:IP, single dose (Pharmacokinetic Analysis)
Result:Had a half-life of 115 min in human plasma, a 2.8-fold increase in stability.
体外研究：
NN-390 exhibits cellular potency with IC50 values of 1.19 μM in MV4-11 cells and 1.38 μM in MM.1S cells while having minimal effects on noncancerous counterparts (IC50 > 50 μM in MRC-9).NN-390 (72 h) strongly decreases proliferation in HD-MB03 cells, with an IC50 of 0.13 μM, and significantly impairs self-renewal of BTIC-enriched HD-MB03s.NN-390 (0-2 μM, 1 h) markedly increases acetylation of α-tubulin and minimally changes acetylated histone H3.NN-390 (6 h) results in acetylation of α-tubulin from concentrations as low as 0.1 μM (0-0.2 μM), and dose-dependent increases in acetylation of α-tubulin (0-0.2 μM).NN-390 (0-2 μM, 24 h) promotes cancer cells apoptosis in MV4-11 cells.
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
体内研究：
NN-390 (male CD-1 mice, 20 mg/kg, IP, single dose) increases plasma stability.NN-390 can improve PAMPA (parallel artificial membrane permeability assay)-BBB (blood-brain barrier) score.Pharmacokinetic Parameters of NN-390 in male male CD-1 mice.CompoundKT-531 5a; NN-390
t1/2 (h)1.051.90
Cmax (ng/mL)493750
AUClast (h*ng/mL)15762523
AUClnf (h*ng/mL)15192548
AUC/D (h*ng/mL)79126
Animal Model:CD-1 mice (male, n=3)
Dosage:20 mg/kg
Administration:IP, single dose (Pharmacokinetic Analysis)
Result:Had a half-life of 115 min in human plasma, a 2.8-fold increase in stability.
体外研究：
NN-390 exhibits cellular potency with IC50 values of 1.19 μM in MV4-11 cells and 1.38 μM in MM.1S cells while having minimal effects on noncancerous counterparts (IC50 > 50 μM in MRC-9).NN-390 (72 h) strongly decreases proliferation in HD-MB03 cells, with an IC50 of 0.13 μM, and significantly impairs self-renewal of BTIC-enriched HD-MB03s.NN-390 (0-2 μM, 1 h) markedly increases acetylation of α-tubulin and minimally changes acetylated histone H3.NN-390 (6 h) results in acetylation of α-tubulin from concentrations as low as 0.1 μM (0-0.2 μM), and dose-dependent increases in acetylation of α-tubulin (0-0.2 μM).NN-390 (0-2 μM, 24 h) promotes cancer cells apoptosis in MV4-11 cells.
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