产品
编 号：F474722
分子式：C28H24F3N7O2
分子量：547.53
分子式：C28H24F3N7O2
分子量：547.53
产品类型
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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结构图
CAS No: 839706-07-9
产品详情
生物活性：
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
体内研究：
GNF-7 (10 -20 mg/kg；op；每天；持续 7 天) 在生物发光异种移植小鼠模型中对 T315I Bcr-Abl 显示出显著的体内功效。口服给药 (小鼠 20 mg/kg) 后，GNF-7 表现出适度的口服生物利用度 (小鼠 36%) 和 Cmax (小鼠 3616 nM)。 由于静脉注射 (小鼠 5 mg/kg) 后的高血浆清除率 (8.6 mL/min/kg)，GNF-7 表现出终末消除半衰期 (小鼠 3.8 小时)。Animal Model:6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage:10 mg/kg, 20 mg/kg
Administration:Oral administration, daily, for 7 days
Result:Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).
Animal Model:5-6 weeks old male Balb/c mice (20-25 g)
Dosage:5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral gavage
Result:Oral bioavailability (36%), Cmax (3616 nM), T1/2 (3.2 h).
体外研究：
GNF-7 有效抑制野生型 Bcr-Abl (IC50GNF-7 相关抗体:Western Blot AnalysisCell Line:Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration:1 μM
Incubation Time:2 hours
Result:Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.
Apoptosis AnalysisCell Line:OCI-AML3 cells
Concentration:1 μM
Incubation Time:24 hours
Result:Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.
Cell Cycle AnalysisCell Line:OCI-AML3 cells
Concentration:1 μM
Incubation Time:24 hours
Result:Induced of G0-G1 arrest.
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
体内研究：
GNF-7 (10 -20 mg/kg；op；每天；持续 7 天) 在生物发光异种移植小鼠模型中对 T315I Bcr-Abl 显示出显著的体内功效。口服给药 (小鼠 20 mg/kg) 后，GNF-7 表现出适度的口服生物利用度 (小鼠 36%) 和 Cmax (小鼠 3616 nM)。 由于静脉注射 (小鼠 5 mg/kg) 后的高血浆清除率 (8.6 mL/min/kg)，GNF-7 表现出终末消除半衰期 (小鼠 3.8 小时)。Animal Model:6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage:10 mg/kg, 20 mg/kg
Administration:Oral administration, daily, for 7 days
Result:Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).
Animal Model:5-6 weeks old male Balb/c mice (20-25 g)
Dosage:5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral gavage
Result:Oral bioavailability (36%), Cmax (3616 nM), T1/2 (3.2 h).
体外研究：
GNF-7 有效抑制野生型 Bcr-Abl (IC50GNF-7 相关抗体:Western Blot AnalysisCell Line:Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration:1 μM
Incubation Time:2 hours
Result:Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.
Apoptosis AnalysisCell Line:OCI-AML3 cells
Concentration:1 μM
Incubation Time:24 hours
Result:Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.
Cell Cycle AnalysisCell Line:OCI-AML3 cells
Concentration:1 μM
Incubation Time:24 hours
Result:Induced of G0-G1 arrest.
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