| 生物活性 | Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor ofEGFR,HER4andHER2, withIC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity[1][2]. |
| IC50& Target[1] | EGFR 1.48 ± 0.0 nM (IC50) | HER4 2.49 ± 0.1 nM (IC50) | HER2 7.15 ± 0.5 nM (IC50) |
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体外研究
(In Vitro) | Epertinib inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50values of 4.5 and 1.6 nM, respectively[2].
Epertinib shows inhibitory activity against MDA-MB-361 cell, with an IC50of 26.5 nM[1].
Epertinib (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2[2].
Cell Proliferation Assay[2] | Cell Line: | NCI-N87 (stomach), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast), and MRC-5 (lung) | | Concentration: | 0-10 μM | | Incubation Time: | 72 h | | Result: | Inhibited the growth of NCI-N87, BT-474, SK-BR-3, MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2, and MRC-5, with IC50values of 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6 ± 4.3, 53.3 ± 8.6, 241.5 ± 29.2, 5366.7 ± 65.2, and 4964.6 ± 340.3. |
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体内研究
(In Vivo) | Epertinib (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity[1].
Epertinib (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume[1].
Epertinib (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner[2].
| Animal Model: | Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1] | | 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 ED50values 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)[1] | | 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)[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
