HER2-IN-9 是一种具有口服活性的HER2抑制剂，IC50值为0.03 μM。HER2-IN-9 抑制 HER-2 阳性的乳腺癌细胞增殖和迁移。HER2-IN-9 可用于乳腺癌研究。
| 生物活性 | HER2-IN-9 is an orally activeHER2inhibitor, with anIC50value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breastcancercells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | HER2-IN-9 (24 h) shows anti-proliferation activities against cancer cells (A549, HEPG2, MCF7, SKBR3)[1].
HER2-IN-9 (0-60 nM, 24 h) inhibits the migration of SKBR3 cells[1].
HER2-IN-9 (0-60 nM, 24 h) increases E-cadherin levels and decreases N-cadherin levels in SKBR3 cells[1].
HER2-IN-9 (0-60 nM, 24 h) suppresses the expression of p-HER-2, further inhibits the activation of the EMT signal pathway to inhibit the migration of SKBR3 cells[1].
Cell Proliferation Assay[1] | Cell Line: | Cancer cells (A549, HEPG2, MCF7, SKBR3), normal cells (Beas2b, LO2, MCF-0A) | | Concentration: | 0.05-30 μM approximately | | Incubation Time: | 24 h | | Result: | Inhibited cancer cell proliferation with IC50s of 0.05-12.17 μM.
Inhibited noamal cell proliferation with IC50s of 15.4- 26.95 μM. |
Western Blot Analysis[1] | Cell Line: | SKBR3 cells | | Concentration: | 0, 20, 40, 60 nM | | Incubation Time: | 24 h | | Result: | Inhibited HER-2 phosphorylation with no significant change in total HER-2 protein levels.
Down-regulated β-catenin, snail, and Vimentin level. |
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体内研究
(In Vivo) | HER2-IN-9 (oral administration, 30 mg/kg, every two days) inhibits tumor growth SKBR3 orthotopic xenograft model[1].
| Animal Model: | SKBR3 orthotopic xenograft model[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration, every two days. | | Result: | Inhibited the growth of cancer cellsin vivowithout noticeable toxic effects.
Increased the level of cleaved-caspase 3 implicated in cell death pathways (immunohistochemistry assay in tumor). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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