Briquilimab  (Synonyms: JSP-191; AMG-191)

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^[1][2].

c-Kit/CD117

Briquilimab (75 μg, i.v., one single dose) significantly depletes low-risk MDS HSCs in the mice model engrafted with HSCs derived from low-risk MDS patients^[3].
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.

3815  [NCBI]

P10721

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

145.61 kDa

2574591-89-0

Liquid

Colorless to light yellow

[Briquilimab]

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG1 kappa

• 
  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.

• [1]. Rajni Agarwal, et al., First Report of Non-Genotoxic Conditioning with JSP191 (anti-CD117) and Hematopoietic Stem Cell Transplantation in a Newly Diagnosed Patient with Severe Combined Immune Deficiency, Blood, Volume 136, Supplement 1, 2020, Page 10, ISSN 0006-4971.

  [2]. Dawoon Jung, et al., Pharmacokinetics of Briquilimab as a Conditioning Agent for Hematopoietic Stem Cell Transplantation in Patients With Severe Combined Immunodeficiency, Myelodysplastic Syndrome, or Acute Myeloid Leukemia, Transplantation and Cellular Therapy, Volume 30, Issue 9, 2024, Pages 923.e1-923.e9, ISSN 2666-6367

  [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]