Lorigerlimab
Based on 1 Customer Validation
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC).
For research use only. We do not sell to patients.
- Purity: 97.5%
- CAS No.: 2416595-46-3
- Molecular Weight:166.4 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
[V-kappa'-VH-h-CH2-CH3_V-kappa-VH']2
Human
CTLA4 & PDCD1
Lorigerlimab (0.01 nM-1 nM) binds to Jurkat/PD-1 cells and blocks PD-L1 binding to the cells[2].
Lorigerlimab can independently engage and block PD-1 and CTLA-4 on cells expressing one or the other checkpoint molecule (EC50: 0.42 nM for PD-1+ cells, 4.8 nM for CTLA-4+ cells, 0.013 nM for PD-1 and CTLA-4+ cells)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lorigerlimab (10-100 mg/kg, i.v., 4 weeks) is well tolerated in cynomolgus monkeys, and shows a half-life about 7 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys [4]
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Dosage:75 mg/kg
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Administration:i.v.
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Result:Increased the Ki67+ T cell fraction, and showed T cell expansion in the spleen.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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[V-kappa'-VH-h-CH2-CH3_V-kappa-VH']2
ELISA, FACS, Functional assay
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Immobilized PD-1 Protein, Human (143a.a, HEK293, His, HY-P7396) can bind Lorigerlimab. The EC50 for this effect is 36.2 ng/mL. -
Immobilized CTLA-4 Protein, Human (HEK293, HY-P72959) can bind Lorigerlimab. The EC50 for this effect is 38.3 ng/mL. -
Flow Cytometry analysis of Raji cells labelling CTLA4 (red) with Lorigerlimab (HY-P99714). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then cells were stained with the primary antibody at 1/200 dilution for an hour at 4℃. Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 (S228P) kappa (HY-P99003, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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CAS No. 2416595-46-3
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Appearance Liquid
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Molecular Weight 166.4 kDa
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Color Colorless to light yellow
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SMILES
[Lorigerlimab]
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Synonyms
MGD019
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (260 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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Inhibitory Antibodies User Guide (603 KB)
References
[2]. Berezhnoy A, et al. Development and Preliminary Clinical Activity of PD-1-Guided CTLA-4 Blocking Bispecific DART Molecule. Cell Rep Med. 2020 Dec 22;1(9):100163. [Content Brief]
[3]. Trojaniello C, Luke JJ, Ascierto PA. Therapeutic Advancements Across Clinical Stages in Melanoma, With a Focus on Targeted Immunotherapy. Front Oncol. 2021 Jun 10;11:670726. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)