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Farletuzumab ecteribulin

本半岛bd体育手机客户端不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2407465-18-1

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

半岛bd体育手机客户端名称

MORAb-202

半岛bd体育手机客户端介绍

Farletuzumab ecteribulin (MORAb-202) 是一种抗体-药物偶联物 ( ADC)，由人源化抗人叶酸受体 α (FRA) 抗体 Farletuzumab (HY-P99153) 通过还原的链间二硫键与 Mal-PEG2-Val-Cit-PAB-eribulin 偶联而成。Farletuzumab ecteribulin 的药物抗体比为 4.0。Farletuzumab ecteribulin 在体外对 FRA 阳性细胞具有高度细胞毒性。Farletuzumab ecteribulin 具有有效的抗肿瘤活性。

生物活性

Farletuzumab ecteribulin (MORAb-202) is anantibody-drug conjugate (ADC), consisting of the humanized anti-humanfolate receptor alpha(FRA) antibodyFarletuzumab (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].

体外研究
(In Vitro)

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:	Human IGROV-1, OVCAR3-A1, NCI-H2110, A431-A3, and SJSA-1 cells
Concentration:	5.1 pM-10 μM
Incubation Time:	5 days
Result:	MORAb-202 showed potent cytotoxicity against IGROV-1 (IC₅₀=1 nM), NCI-H2110 (IC₅₀=74 nM), and A431-A3 (IC₅₀=2.3 μM). Exhibited little killing activity against the FRA-negative cell line SJSA-1 (IC₅₀>10 μM).

体内研究
(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 T_1/2分别为 192 和 162 小时，AUC_(0-t)分别为 7160 和 6300 ug·h/mL^[1]。

Animal Model:	Female SWISS nude mice with triple-negative breast cancer (TNBC) patient-derived xenograft (PDx) model (OD-BRE-0631)^[1].
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^[1].
Dosage:	2mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2s 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.

CAS 号

2407465-18-1

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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