产品
编 号：F205748
分子式：C25H30N8O4
分子量：506.56
分子式：C25H30N8O4
分子量：506.56
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1708971-55-4
产品详情
生物活性：
Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
体内研究：
Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days.Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) . Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min?kg, and a Vss of 3.9 L/kg for male SD rats. Animal Model:Male Wistar Hannover rats (Hep3B xenograft model)
Dosage:10, 30, 100 mg/kg
Administration:Gavage; for 10 days
Result:Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
Animal Model:Male mice (C57BL/6)
Dosage:1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis)
Administration:IV at 1 mg/kg; PO at 3 mg/kg
Result:Had a T1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a Vss of 2.3 L/kg.
体外研究：
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC50= 1.9 nM). Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM). Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM).
Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
体内研究：
Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days.Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) . Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min?kg, and a Vss of 3.9 L/kg for male SD rats. Animal Model:Male Wistar Hannover rats (Hep3B xenograft model)
Dosage:10, 30, 100 mg/kg
Administration:Gavage; for 10 days
Result:Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
Animal Model:Male mice (C57BL/6)
Dosage:1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis)
Administration:IV at 1 mg/kg; PO at 3 mg/kg
Result:Had a T1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a Vss of 2.3 L/kg.
体外研究：
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC50= 1.9 nM). Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM). Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM).
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