产品
编 号：F168523
分子式：C25H25BrN6O2
分子量：521.41
分子式：C25H25BrN6O2
分子量：521.41
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1457983-28-6
产品详情
生物活性：
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML).
体内研究：
Denfivontinib (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models.Animal Model:Athymic nu/nu mice, subcutaneous MV4-11 xenograft mice
Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:Oral administration, daily, for 28 days
Result:Suppressed tumor growth.
体外研究：
Denfivontinib shows potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.Denfivontinib inhibits autophosphorylation of FLT3 with an IC50 value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells.Denfivontinib (0.0001-10 nM; 72 hours) shows strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner.Denfivontinib (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis.Denfivontinib (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412.
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML).
体内研究：
Denfivontinib (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models.Animal Model:Athymic nu/nu mice, subcutaneous MV4-11 xenograft mice
Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:Oral administration, daily, for 28 days
Result:Suppressed tumor growth.
体外研究：
Denfivontinib shows potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.Denfivontinib inhibits autophosphorylation of FLT3 with an IC50 value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells.Denfivontinib (0.0001-10 nM; 72 hours) shows strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner.Denfivontinib (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis.Denfivontinib (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412.
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