产品
编 号：F741503
分子式：C24H22N6O4
分子量：458.47
分子式：C24H22N6O4
分子量：458.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2320462-65-3
产品详情
生物活性：
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
体内研究：
HPK1-IN-7 (compound 24) (100 mg/kg; p.o.; twice daily for 28 days) 在结直肠癌同系肿瘤模型中显示抗 PD1 功效的强劲增强。 HPK1-IN-7 (1 mg/kg; intravenous; mice) 的特点是血浆清除率适中 (43 mL/min/kg) 和分布容积大 (4.4 L/kg)。口服 (20 mg/kg) 后，Cmax 为 5.3 μM，AUC0-24h为 19 μM?h。根据这些药代动力学研究计算出的口服生物利用度约为 100%。Animal Model:Mice (MC38 syngeneic tumor model)
Dosage:100 mg/kg
Administration:Oral; twice daily for 28 days
Result:Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone.
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
体内研究：
HPK1-IN-7 (compound 24) (100 mg/kg; p.o.; twice daily for 28 days) 在结直肠癌同系肿瘤模型中显示抗 PD1 功效的强劲增强。 HPK1-IN-7 (1 mg/kg; intravenous; mice) 的特点是血浆清除率适中 (43 mL/min/kg) 和分布容积大 (4.4 L/kg)。口服 (20 mg/kg) 后，Cmax 为 5.3 μM，AUC0-24h为 19 μM?h。根据这些药代动力学研究计算出的口服生物利用度约为 100%。Animal Model:Mice (MC38 syngeneic tumor model)
Dosage:100 mg/kg
Administration:Oral; twice daily for 28 days
Result:Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone.
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