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Farletuzumab ecteribulin

Cat. No. M25118
Farletuzumab ecteribulin Structure
Synonym:

MORAb-202

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Biological Activity

Farletuzumab ecteribulin (MORAb-202) is an antibody-drug conjugate (ADC), consisting of the humanized anti-human folate receptor alpha (FRA) antibody Farletuzumab 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.

Chemical Information
CAS Number 2407465-18-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Toshio Shimizu, et al. Clin Cancer Res. First-in-Human Phase 1 Study of MORAb-202, an Antibody-Drυg Conjugate Comprising Farletuzumab Linked to Eribulin Mesylate, in Patients with Folate Receptor-α-Positive Advanced Solid Tumors

[2] Mariana Scaranti, et al. Nat Rev Clin Oncol. Exploiting the folate receptor α in oncology

[3] Xin Cheng, et al. Mol Cancer Ther. MORAb-202, an Antibody-Drυg Conjugate Utilizing Humanized Anti-human FRα Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity

[4] Seiya Sato, et al. Onco Targets Ther. Profile of farletuzumab and its potential in the treatment of solid tumors

[5] Anish Thomas, et al. Lung Cancer. Farletuzumab in lung cancer

Related Drug-Linker Conjugates for ADC Products
SC-VC-PAB-MMAE

SC-VC-PAB-MMAE is part of a drug-linker conjugate for ADC (ADC) with anticancer activity, which consists of MMAE (a tubulin inhibitor) linked to a cleavable SC-VC-PAB linker.

DBCO-(PEG)3-VC-PAB-MMAE

DBCO-(PEG)3-vc-PAB-MMAE is an active molecule coupler (drug-linker conjugate for ADC) consisting of auristatin E attached to a DBCO-(PEG)3-vc-PAB connector. It can be used for cancer research. In addition, DBCO-(PEG)3-vc-PAB-MMAE is a click chemistry that contains a DBCO moiety and can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing an Azide moiety.

PB038

PB038 is a drug-liker containing a PEG unit and a cleavable linker attached to Exatecan.

Val-Ala-PAB-MMAE

Val-Ala-PAB-MMAE is a Drug-Linker Conjugate for ADC, consisting of ADC linker (Val-Ala-PAB) and MMAE.

Val-Ala-PABC-Exatecan

Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor).

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Keywords: Farletuzumab ecteribulin, MORAb-202 supplier, Drug-Linker Conjugates for ADC, inhibitors, activators


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