| Bioactivity | Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload[1][2]. |
| Invitro | Aprutumab ixadotin (0.097-0.83 nM; 72 h) 对 FGFR2 表现出 0.29 nM 的抗原结合亲和力，并在几个癌细胞系中表现出抑制活性，IC50 为 0.097-0.83 nM[1]。Aprutumab ixadotin 还诱导 FGFR2 阳性细胞凋亡 (SUN-52PE, SUN-16)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Aprutumab ixadotin 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | Aprutumab ixadotin (5 mg/kg 或 7.5 mg/kg; 静脉注射; 每周一次, 共 30 天) 耐受性良好，可导致小鼠中 SNU-16、MFM-223 或 NCI-H716 异种移植物模型肿瘤部分消退[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1708947-48-1 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sommer A, et al. Preclinical Efficacy of the Auristatin-Based Antibody-Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors. Cancer Res. 2016 Nov 1;76(21):6331-6339. [2]. Kim SB, et al. First-in-Human Phase I Study of Aprutumab Ixadotin, a Fibroblast Growth Factor Receptor 2 Antibody-Drug Conjugate (BAY 1187982) in Patients with Advanced Cancer. Target Oncol. 2019 Oct;14(5):591-601. |