产品
编 号：F752077
分子量：149000
分子量：149000
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2407465-18-1
产品详情
生物活性：
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 agent-to-antibody ratio of 4.0. Farletuzumab ecteribulin is highly cytotoxic to FRA-positive cells in vitro. Farletuzumab ecteribulin has potent antitumor activity.
体内研究：
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。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。Animal Model:Female SWISS nude mice with triple-negative breast cancer (TNBC) patient-derived xenograft (PDx) model (OD-BRE-0631).
Dosage:1, 5 mg/kg
Administration:IV; single injection 1, 5?mg/kg at day 0 ((Q1Dx1) or 5?mg/kg every 11 days (Q11Dx2)); 60 days
Result:A significant antitumor activity was observed in mice treated once or twice 5 mg/kg, while no antitumor activity compared with vehicle group was observed in mice treated with 1 mg/kg.
Animal Model:Male and female cynomolgus monkeys.
Dosage:2mg/kg (Pharmacokinetic?Analysis)
Administration:IV
Result:Had a T1/2s of 192 and 162 hours and AUC(0-t)s of 7160 and 6300 ug·h/mL for male and female cynomolgus monkeys on Day 1.
体外研究：
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)。
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 agent-to-antibody ratio of 4.0. Farletuzumab ecteribulin is highly cytotoxic to FRA-positive cells in vitro. Farletuzumab ecteribulin has potent antitumor activity.
体内研究：
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。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。Animal Model:Female SWISS nude mice with triple-negative breast cancer (TNBC) patient-derived xenograft (PDx) model (OD-BRE-0631).
Dosage:1, 5 mg/kg
Administration:IV; single injection 1, 5?mg/kg at day 0 ((Q1Dx1) or 5?mg/kg every 11 days (Q11Dx2)); 60 days
Result:A significant antitumor activity was observed in mice treated once or twice 5 mg/kg, while no antitumor activity compared with vehicle group was observed in mice treated with 1 mg/kg.
Animal Model:Male and female cynomolgus monkeys.
Dosage:2mg/kg (Pharmacokinetic?Analysis)
Administration:IV
Result:Had a T1/2s of 192 and 162 hours and AUC(0-t)s of 7160 and 6300 ug·h/mL for male and female cynomolgus monkeys on Day 1.
体外研究：
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)。
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