产品
编 号：F752225
分子式：C29H25FN4O4
分子量：512.53
分子式：C29H25FN4O4
分子量：512.53
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CAS No: 2411379-14-9
产品详情
生物活性：
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
体内研究：
HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg.HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity.Animal Model:Female BALB/C nude mice (5-6 weeks, 18-20 g; injected with human K562 cells)
Dosage:5 and 10 mg/kg
Administration:PO; daily, for 14 days
Result:Exhibited potent oral antitumor activity at 5 mg/kg with a TGI value of 41.4% and a T/C value of 54.3%, and achieved better tumor growth inhibition with a TGI of 68.5% and a T/C of 25.5%.
体外研究：
HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines.HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells.HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner.HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase.
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
体内研究：
HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg.HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity.Animal Model:Female BALB/C nude mice (5-6 weeks, 18-20 g; injected with human K562 cells)
Dosage:5 and 10 mg/kg
Administration:PO; daily, for 14 days
Result:Exhibited potent oral antitumor activity at 5 mg/kg with a TGI value of 41.4% and a T/C value of 54.3%, and achieved better tumor growth inhibition with a TGI of 68.5% and a T/C of 25.5%.
体外研究：
HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines.HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells.HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner.HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase.
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