| Size | Price | |
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| 1mg | ||
| Other Sizes |
| ln Vitro |
In vitro, farletuzumab ecteribulin (MORAb-202; 5.1 pM-10 μM; 5 days) exhibits strong cytotoxicity towards FRA-positive cells (IC50 = 1 nM for IgV-1, IC50 = 74 nM for NCI-H2110, and IC50 = 2.3 μM for A431-2A3)[1].
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| ln Vivo |
Farletuzumab ecteribulin (MORAb-202; IV; 1, 5 mg/kg as a single injection on Day 0; or 5 mg/kg every 11 days for 2 doses; 60 days) 5 mg/kg once or twice It exhibits noteworthy anti-tumor effectiveness at kg dose[1]. The first-day AUC(0-t) of farletuzumab ecteribulin (2 mg/kg; i.v.) in male and female cynomolgus monkeys was 7160 and 6300 ug·h/mL, respectively, with T1/2 of 192 and 162 hours [1].
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Human IGROV-1, OVCAR3-A1, NCI-H2110, A431-A3, and SJSA -1 cells Tested Concentrations: 5.1 pM-10 μM Incubation Duration: 5 days Experimental Results: MORAb-202 demonstrated potent cytotoxicity against IGROV-1 (IC50=1 nM), NCI-H2110 (IC50=74 nM), and A431-A3 (IC50 =2.3 μM). demonstrated little killing activity against the FRA-negative cell line SJSA-1 (IC50>10 μM). |
| Animal Protocol |
Animal/Disease Models: Female SWISS nude mice with triple-negative breast cancer (TNBC) patient-derived xenograft (PDx) model (OD-BRE-0631)[1].
Doses: 1, 5 mg/kg Route of Administration: IV; single injection 1, 5 mg/kg at day 0 ((Q1Dx1) or 5 mg/kg every 11 days (Q11Dx2)); 60 days Experimental Results: 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/Disease Models: Male and female cynomolgus monkeys[1]. Doses: 2mg/kg ( pharmacokinetic/PK Analysis) Route of Administration: IV Experimental Results: Had a T1/2s of 192 and 162 hrs (hours) and AUC(0-t)s of 7160 and 6300 ug·h/mL for male and female cynomolgus monkeys on Day 1. |
| 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.
[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. |
| CAS # |
2407465-18-1
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|---|---|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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