| Bioactivity | Farletuzumab ecteribulin (MORAb-202) is an antibody-drug conjugate (ADC), consisting of the humanized anti-human folate receptor alpha (FRA) antibody Farletuzumab (HY-P99153) conjugated via reduced interchain disulfide bonds to Mal-PEG2-Val-Cit-PAB-eribulin. Farletuzumab ecteribulin has a drug-to-antibody ratio of 4.0. Farletuzumab ecteribulin is highly cytotoxic to FRA-positive cells in vitro. Farletuzumab ecteribulin has potent antitumor activity[1][2]. |
| Invitro | Farletuzumab ecteribulin (MORAb-202; 5.1 pM-10 μM; 5 天) 在体外对 FRA 阳性细胞具有高度细胞毒性 (IGROV-1: IC50=1 nM, NCI-H2110: IC50=74 nM, A431-A3: IC50=2.3 μM)[1]。 Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | Farletuzumab ecteribulin (MORAb-202; 静脉给药; 第 0 天单次注射 1, 5 mg/kg; 或每 11 天注射一次 5 mg/kg, 共2次; 60 天) 在一次或两次 5 mg/kg 剂量下具有显着的抗肿瘤活性[1]。Farletuzumab ecteribulin (2mg/kg; 静脉给药) 第 1 天在雄性和雌性食蟹猴中的 T1/2 分别为 192 和 162 小时，AUC(0-t) 分别为 7160 和 6300 ug·h/mL[1]。 Animal Model: |
| Name | Farletuzumab ecteribulin |
| CAS | 2407465-18-1 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Keiji Furuuchi, et al. Antibody-drug conjugate MORAb-202 exhibits long-lasting antitumor efficacy in TNBC PDx models. Cancer Sci. 2021 Jun;112(6):2467-2480. [2]. Xin Cheng, et al. MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FRα Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018 Dec;17(12):2665-2675. |