Bioactivity | Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models[1]. |
Invitro | Seribantumab (0.1 nmol/L-10 μmol/L; 96 h) 剂量依赖性地抑制两种神经调节蛋白 1 (NRG1) 重排的融合细胞系 (MDA-MB-175-VII、DOC4-NRG1 融合和 LUAD-0061AS3、SLC3A2-NRG1 融合),抑制 MDA-MB-175-VII、LUAD-0061AS3、MCF-7 和 HBECp53 细胞的 IC50 值分别为 0.02、1.4、45.2 和 203 μmol/L[1]。Seribantumab (0.1, 1 and 10 μmol/L; 24-48 h) 有效抑制 NRG1 融合或 NRG1 扩增的肿瘤细胞系的生长[1]。Seribantumab (0-0.5 μmol/L; 96 h) 强烈抑制 NRG1-b1 刺激的 MCF-7 细胞的生长[1]。Seribantumab (0-10 μmol/L; 48 h) 诱导 NRG1 重排细胞的凋亡[1]。Seribantumab (0-10 μmol/L; 1 h) 抑制 NRG1 下游调节因子的磷酸化[1]。 Apoptosis Analysis[1] Cell Line: |
In Vivo | Seribantumab (0.6-1 mg;腹腔注射,两周一次,共注射一次) 比阿法替尼更有效地减少非小细胞肺癌肿瘤生长,阻断生长调节因子的磷酸化并诱导细胞凋亡标志物的表达[1]。Seribantumab (1-10 mg;腹腔注射,两周一次,共注射一次) 在高级别浆液性卵巢癌 (HGSOC) 小鼠模型中,可以消除绝大多数肿瘤细胞,并且对动物健康或体重没有显著变化[1]。 Animal Model: |
Name | Seribantumab |
CAS | 1334296-12-6 |
Molar Mass | 143.2 (kDa) |
Appearance | Liquid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Odintsov I, et al. The Anti-HER3 mAb Seribantumab Effectively Inhibits Growth of Patient-Derived and Isogenic Cell Line and Xenograft Models with Oncogenic NRG1 Fusions. Clin Cancer Res. 2021 Jun 1;27(11):3154-3166. |