产品
编 号：F193407
分子式：C20H26Cl2N4O3S
分子量：473.42
分子式：C20H26Cl2N4O3S
分子量：473.42
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CAS No: 1613439-62-5
产品详情
生物活性：
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
体内研究：
PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models.PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose.PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor.PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/? p53?/? medulloblastoma mice.PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T1/2) of 1.7±0.1 hours.Animal Model:Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered
Dosage:0, 1, 5, 10, 30 mg/kg
Administration:P.o. once daily for 6 days
Result:Showed robust antitumor activity with an in vivo IC50 of 8.9±2.6 nM.
Animal Model:Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old)
Dosage:0, 5, 10, 30 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:The apparent volume of distribution of 5.6±0.5 L/kg; the half-life (T1/2) of 1.7±0.1 hours.
体外研究：
PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC50 of 2.7±1.4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells.PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM.
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
体内研究：
PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models.PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose.PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor.PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/? p53?/? medulloblastoma mice.PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T1/2) of 1.7±0.1 hours.Animal Model:Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered
Dosage:0, 1, 5, 10, 30 mg/kg
Administration:P.o. once daily for 6 days
Result:Showed robust antitumor activity with an in vivo IC50 of 8.9±2.6 nM.
Animal Model:Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old)
Dosage:0, 5, 10, 30 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:The apparent volume of distribution of 5.6±0.5 L/kg; the half-life (T1/2) of 1.7±0.1 hours.
体外研究：
PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC50 of 2.7±1.4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells.PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM.
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