| 名称 | AV-412 |
| 描述 | AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively. |
| 体外活性 | In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
| 体内活性 | In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth in A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed EGFR and ErbB2 autophosphorylation at doses corresponding to its antitumor efficacy. Various dosing schedules showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting frequent dosing is preferable. Additionally, MP-412 exhibited significant antitumor effects on the ErbB2-overexpressing KPL-4 breast cancer cell line, which is resistant to gefitinib. These studies indicate MP-412's potential as a therapeutic for cancers expressing EGFR and ErbB2, especially those resistant to first-generation small-molecule inhibitors. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 25 mg/mL (29.36 mM)
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| 关键字 | EGFR | Inhibitor | inhibit | MP 412 | HER1 | Epidermal growth factor receptor | AV-412 | AV412 | AV 412 | MP-412 | ErbB-1 |
| 相关产品 | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| 相关库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
