产品
编 号：F752727
分子式：C22H23ClFN5O2
分子量：443.9
分子式：C22H23ClFN5O2
分子量：443.9
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CAS No: 2435562-99-3
产品详情
生物活性：
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia.
体内研究：
FLT3-IN-15 (20 mg/kg; PO; daily, for 21 days) results in the rapid and complete remission of tumors in all mice.FLT3-IN-15 (2000 mg/kg; PO; single) causes one female mouse died at day 6, and the LD50 value is calculated as 4,950 mg/kg in female mice.FLT3-IN-15 (10 μM) shows 21.4% inhibition of hERG ligand binding.FLT3-IN-15 (10 mg/kg; PO and IV; single) exhibits an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.Pharmacokinetic Parameters of FLT3-IN-15 in male ICR mice.PO (10 mg/kg) IV (10 mg/kg)
AUClast (μg·min/mL)25.0 ± 11.658.5 ± 57.4
AUCinf (μg·min/mL)62.1 ± 58.6103.4 ± 95.3
MRT (hr)2811.3 ± 2713.01257.1 ± 1084.1
T1/2 (hr)1775.7 ± 1901.01099.2 ± 945.8
CL (mL/min/kg)158.7 ± 98.7
VSS (L/kg)127891 ± 104764
Cmax (ng/mL)36.5 ± 24.3
Tmax (min)390.0 ± 366.0
Xu, 24h (%)0.001 ± 0.00.002 ± 0.002
GI24h (%)0.05 ± 0.050.24 ± 0.02
F (%)42.9
Animal Model:BALB/c nu/nu (injected with MV4-11)
Dosage:20 mg/kg
Administration:PO; daily, for 21 days
Result:Resulted in the rapid and complete remission of tumors in all mice, and no weight loss or any other signs of toxicity during the administration period.
Animal Model:Female ICR mice
Dosage:2000 mg/kg
Administration:PO; single
Result:Caused one female mouse of the 2,000?mg/kg group died at day 6 and the approximate lethal dose (ALD) is determined over 2,000?mg/kg in male mice and 2,000?mg/kg in female mice, respectively; the LD50 value was calculated as 4,950 mg/kg in female mice.
Animal Model:Male ICR mice
Dosage:10 mg/kg
Administration:PO and IV; single (Pharmacokinetics Analysis)
Result:Exhibited an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.
体外研究：
FLT3-IN-15 (compound 36) (0-100 nM) exhibits anti-proliferative activities against MOLM14 cell lines.FLT3-IN-15 (0-1 μM; 72 hours) shows extremely more sensitive against MV4-11?cells than K562?cell line, and displayed good safety profiles against other cancer cell lines.FLT3-IN-15 (0.01-1 μM; 4 hours) shows strongly blockage of the phosphorylation of STAT5 and Erk1/2 in MV4-11 cells.
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia.
体内研究：
FLT3-IN-15 (20 mg/kg; PO; daily, for 21 days) results in the rapid and complete remission of tumors in all mice.FLT3-IN-15 (2000 mg/kg; PO; single) causes one female mouse died at day 6, and the LD50 value is calculated as 4,950 mg/kg in female mice.FLT3-IN-15 (10 μM) shows 21.4% inhibition of hERG ligand binding.FLT3-IN-15 (10 mg/kg; PO and IV; single) exhibits an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.Pharmacokinetic Parameters of FLT3-IN-15 in male ICR mice.PO (10 mg/kg) IV (10 mg/kg)
AUClast (μg·min/mL)25.0 ± 11.658.5 ± 57.4
AUCinf (μg·min/mL)62.1 ± 58.6103.4 ± 95.3
MRT (hr)2811.3 ± 2713.01257.1 ± 1084.1
T1/2 (hr)1775.7 ± 1901.01099.2 ± 945.8
CL (mL/min/kg)158.7 ± 98.7
VSS (L/kg)127891 ± 104764
Cmax (ng/mL)36.5 ± 24.3
Tmax (min)390.0 ± 366.0
Xu, 24h (%)0.001 ± 0.00.002 ± 0.002
GI24h (%)0.05 ± 0.050.24 ± 0.02
F (%)42.9
Animal Model:BALB/c nu/nu (injected with MV4-11)
Dosage:20 mg/kg
Administration:PO; daily, for 21 days
Result:Resulted in the rapid and complete remission of tumors in all mice, and no weight loss or any other signs of toxicity during the administration period.
Animal Model:Female ICR mice
Dosage:2000 mg/kg
Administration:PO; single
Result:Caused one female mouse of the 2,000?mg/kg group died at day 6 and the approximate lethal dose (ALD) is determined over 2,000?mg/kg in male mice and 2,000?mg/kg in female mice, respectively; the LD50 value was calculated as 4,950 mg/kg in female mice.
Animal Model:Male ICR mice
Dosage:10 mg/kg
Administration:PO and IV; single (Pharmacokinetics Analysis)
Result:Exhibited an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.
体外研究：
FLT3-IN-15 (compound 36) (0-100 nM) exhibits anti-proliferative activities against MOLM14 cell lines.FLT3-IN-15 (0-1 μM; 72 hours) shows extremely more sensitive against MV4-11?cells than K562?cell line, and displayed good safety profiles against other cancer cell lines.FLT3-IN-15 (0.01-1 μM; 4 hours) shows strongly blockage of the phosphorylation of STAT5 and Erk1/2 in MV4-11 cells.
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