Farletuzumab ecteribulin
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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.
For research use only. We do not sell to patients.
- Purity : 98.97%
- CAS No.: 2407465-18-1
- Molecular Weight:149000 (average)
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Storage:
-80°C, protect from light
Biological Activity
Description
In Vitro
Farletuzumab ecteribulin (MORAb-202; 5.1 pM-10 μM; 5 days) is highly cytotoxic to FRA-positive cells in vitro (IGROV-1: IC50=1 nM, NCI-H2110: IC50=74 nM, A431-A3: IC50=2.3 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human IGROV-1, OVCAR3-A1, NCI-H2110, A431-A3, and SJSA-1 cells
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Concentration:5.1 pM-10 μM
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Incubation Time:5 days
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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).
In Vivo
Farletuzumab ecteribulin (2mg/kg; IV) has 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SWISS nude mice with triple-negative breast cancer (TNBC) patient-derived xenograft (PDx) model (OD-BRE-0631)[1].
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Dosage:1, 5 mg/kg
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Administration:IV; single injection 1, 5 mg/kg at day 0 ((Q1Dx1) or 5 mg/kg every 11 days (Q11Dx2)); 60 days
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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.
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Animal Model:Male and female cynomolgus monkeys[1].
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Dosage:2mg/kg (Pharmacokinetic Analysis)
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Administration:IV
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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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2407465-18-1
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Appearance Liquid
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Molecular Weight 149000 (average)
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Color Colorless to light yellow
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SMILES
[Farletuzumab ecteribulin]
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Synonyms
MORAb-202
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)