Farletuzumab ecteribulin
Based on 1 Customer Validation
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.
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- Pureté: 98.97%
- CAS No.: 2407465-18-1
- Masse moléculaire:149000 (average)
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Stockage:
-80°C, protect from light
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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).
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| 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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Masse moléculaire 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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Livraison
Shipping with dry ice.
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Stockage
-80°C, protect from light
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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)
Farletuzumab ecteribulin Related Classifications
HY-P99612 Related Classifications
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