1. Antibody-drug Conjugate/ADC Related
  2. Antibody-Drug Conjugates (ADCs)
  3. Farletuzumab ecteribulin

Farletuzumab ecteribulin  (Synonyms: MORAb-202)

目录号: HY-P99612

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。

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Farletuzumab ecteribulin Chemical Structure

Farletuzumab ecteribulin Chemical Structure

CAS No. : 2407465-18-1

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  • 生物活性

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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 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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 T1/2 分别为 192 和 162 小时,AUC(0-t) 分别为 7160 和 6300 ug·h/m[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 T1/2s of 192 and 162 hours and AUC(0-t)s of 7160 and 6300 ug·h/mfor male and female cynomolgus monkeys on Day 1.
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纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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