Briquilimab
Based on 1 Customer Validation
Briquilimab (JSP-191 or AMG-191) is a humanized IgG1 monoclonal antibody that binds human CD117 (c-Kit). Briquilimab blocks the interaction between CD117 receptor and stem cell factor on various CD117 expressing tissues. Briquilimab can lead to inhibition of SCF/c-Kit signaling and MC apoptosis. Briquilimab is a non-toxic approach to target and deplete HSC, enabling blood and immune reconstitution with minimal toxicity with the other agents being used for transient immune suppression to prevent immunologic rejection. Briquilimab can be used in various disease research such as severe combined immunodeficiency (SCID), myelodyplastic syndromes (MDS), acute myeloid leukemia (AML), chronic spontaneous urticarial (CSU), chronic inducible urticarial (CIndU) and asthema.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 2574591-89-0
- Molecular Weight:145.61 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Human IgG1 kappa
Human
c-Kit/CD117
Briquilimab (0.3-1 mg/kg, i.v., one single dose) depletes human HSPCs in all animals after 2 weeks, but the levels of depletion varies among NSG mice model[4].
Briquilimab (0.1-25 mg/kg, i.v., one single dose) has no adverse clinical observations in immunocompetent juvenile cynomolgus macaques[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human CD34+ hematopoietic stem cell-engrafted humanized NSG mice (hu-CD34 NSG, 10-11 weeks old)[1]
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Dosage:0.3 and 1.0 mg/kg
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Administration:Intravenous injection (i.v.), one single dose
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Result:Decreased the ratio of human CD45+/mouse CD45+ in most mice.
Decreased the frequency of human myeloid and T cells.
Increased the frequency of B cells.
Results in gene-marked second human donor cells among hCD45+hCD34+ and hCD45+hCD19+ cell in all mice treated with Briquilimab but not in unconditioned mice, suggesting that Briquilimab conditioning permitted second donor HSPC engraftment.
Led to higher donor chimerism in mice treated with 1.0 mg/kg dose.
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Animal Model:Juvenile 37-39 months old male cynomolgus macaques (3.4−4.0 kg)[4]
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Dosage:0.1, 1, 5, or 25 mg/kg
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Administration:Intravenous injection (i.v.), one single dose
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Result:Resulted in HSPC depletion lasted up to 21 days in most animals and >42 days in animal that received the highest dose.
Caused delayed HSPC recovery with high doses.
| 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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Human IgG1 kappa
ELISA, FACS, Functional assay
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Loaded Briquilimab on AHC2 biosensor, can bind CD117/c-kit Protein, Human (HEK293, His, HY-P72752) with an affinity constant of 5.634E-09 M as determined in BLI assay. -
Immobilized Human c-Kit Protein (ECD, His Tag) can bind Briquilimab. The EC50 for this effect is 1.72 ng/mL. -
Flow Cytometry analysis of THP-1 cells labelling c-Kit/CD117 (red) with Briquilimab (HY-P99488). 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 IgG1 kappa (HY-P99001, 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. 2574591-89-0
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Appearance Liquid
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Molecular Weight 145.61 kDa
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Color Colorless to light yellow
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SMILES
[Briquilimab]
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Synonyms
JSP-191; AMG-191
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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 (262 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
[3]. Pang, W. W., et al., (2019). Anti-CD117 antibody depletes normal and myelodysplastic syndrome human hematopoietic stem cells in xenografted mice. Blood, 133(19), 2069–2078. [Content Brief]
[4]. Kwon, H. S., et al., (2019). Anti-human CD117 antibody-mediated bone marrow niche clearance in nonhuman primates and humanized NSG mice. Blood, 133(19), 2104–2108. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)