产品
编 号：F254276
分子式：C30H28Cl2FN5O3
分子量：596.48
分子式：C30H28Cl2FN5O3
分子量：596.48
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2071195-74-7
产品详情
生物活性：
Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity.Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume.Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner.Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)
Dosage:12.5, 25, 50, 100 ?mg/kg
Administration:Orally, once daily for 28 days
Result:Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1?mg/kg and 26.5?mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively).
Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)
Dosage:50 mg/kg
Administration:Orally, once daily for 30 days
Result:Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier).
Animal Model:Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)
Dosage:0, 6.25, 12.5, 25, and 50 mg/kg
Administration:Oral gavage, daily for 10-28 days
Result:Significantly inhibited the tumor growth in a dose-dependent manner.
体外研究：
Epertinib hydrochloride inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively.Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM.Epertinib hydrochloride (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2.
Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity.Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume.Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner.Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)
Dosage:12.5, 25, 50, 100 ?mg/kg
Administration:Orally, once daily for 28 days
Result:Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1?mg/kg and 26.5?mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively).
Animal Model:Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)
Dosage:50 mg/kg
Administration:Orally, once daily for 30 days
Result:Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier).
Animal Model:Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)
Dosage:0, 6.25, 12.5, 25, and 50 mg/kg
Administration:Oral gavage, daily for 10-28 days
Result:Significantly inhibited the tumor growth in a dose-dependent manner.
体外研究：
Epertinib hydrochloride inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively.Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM.Epertinib hydrochloride (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2.
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