产品
编 号：F763036
分子式：C44H49N13O6
分子量：855.94
分子式：C44H49N13O6
分子量：855.94
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CAS No: 2892631-70-6
产品详情
生物活性：
PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia.
体内研究：
PF15 (10 or 20 mg/kg; i.p.; once daily for 10 days) shows good tumor growth inhibition with an inhibitory rate of 58.4% at dosage of 10 mg/kg, and when up to 20 mg/kg displays higher inhibitory rate.PF15 (twice daily (20 mg/kg), once daily (40 mg/kg); 12 days; i.p.) prolongs the median survival up to 15 days (negative control group is 11 days) in BaF3-FLT3-ITD in situ model.Animal Model:Female NOD/SCID mice (BaF3-FLT3-ITD xenograft model).
Dosage:10 or 20 mg/kg
Administration:Intraperitoneal injection; once daily for 10 days.
Result:Achieved good tumor growth inhibition with an inhibitory rate of 58.4% (10 mg/kg), meanwhile, when at 20 mg/kg displayed higher inhibitory rate.Hardly caused side effects on heart, liver, and kidney (both of the treatment groups).
Animal Model:Female BALB/c nude mice (BaF3-FLT3-ITD in situ model).
Dosage:20, 40 mg/kg
Administration:Intraperitoneal injection; twice daily (20 mg/kg), once daily (40 mg/kg); 12 days.
Result:Prolonged the median survival from 11days to 15 days (both of the treatment groups).
体外研究：
PF15 (0-1000 nM; 72 h) shows good anti-proliferation activity in MV4-11, Molm-13 and BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations).PF15 (1, 3, 10, 30, 100, 300, 1000 nM; 6 h) obviously induces FLT3 degradation in a dose-dependent manner and (10, 30, 100, 300, 1000 nM; 6 h) dramatically inhibits the phosphorylation of FLT3 and STAT5 in BaF3-FLT3-ITD cells.PF15 (10, 30, 100, 300, 1000 nM; 6 h) sharply downregulates the phosphorylation of FLT3 and STAT5 at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells.PF15 (100 nM; 1, 3, 6, 12, 24 h) induces FLT3 degradation in a time-dependent manner from 1 h to 24 h.PF15 (15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM; 24 h) induces FLT3 degradation with a DC50 of 76.7 nM.
PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia.
体内研究：
PF15 (10 or 20 mg/kg; i.p.; once daily for 10 days) shows good tumor growth inhibition with an inhibitory rate of 58.4% at dosage of 10 mg/kg, and when up to 20 mg/kg displays higher inhibitory rate.PF15 (twice daily (20 mg/kg), once daily (40 mg/kg); 12 days; i.p.) prolongs the median survival up to 15 days (negative control group is 11 days) in BaF3-FLT3-ITD in situ model.Animal Model:Female NOD/SCID mice (BaF3-FLT3-ITD xenograft model).
Dosage:10 or 20 mg/kg
Administration:Intraperitoneal injection; once daily for 10 days.
Result:Achieved good tumor growth inhibition with an inhibitory rate of 58.4% (10 mg/kg), meanwhile, when at 20 mg/kg displayed higher inhibitory rate.Hardly caused side effects on heart, liver, and kidney (both of the treatment groups).
Animal Model:Female BALB/c nude mice (BaF3-FLT3-ITD in situ model).
Dosage:20, 40 mg/kg
Administration:Intraperitoneal injection; twice daily (20 mg/kg), once daily (40 mg/kg); 12 days.
Result:Prolonged the median survival from 11days to 15 days (both of the treatment groups).
体外研究：
PF15 (0-1000 nM; 72 h) shows good anti-proliferation activity in MV4-11, Molm-13 and BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations).PF15 (1, 3, 10, 30, 100, 300, 1000 nM; 6 h) obviously induces FLT3 degradation in a dose-dependent manner and (10, 30, 100, 300, 1000 nM; 6 h) dramatically inhibits the phosphorylation of FLT3 and STAT5 in BaF3-FLT3-ITD cells.PF15 (10, 30, 100, 300, 1000 nM; 6 h) sharply downregulates the phosphorylation of FLT3 and STAT5 at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells.PF15 (100 nM; 1, 3, 6, 12, 24 h) induces FLT3 degradation in a time-dependent manner from 1 h to 24 h.PF15 (15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM; 24 h) induces FLT3 degradation with a DC50 of 76.7 nM.
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