Anzurstobart  (Synonyms: CC-95251; BMS-986351)

Anzurstobart is a CD47/SIRPα inhibitor with human SIRPα K_d of 0.0541 nM and human SIRPα IC₅₀ of 100 nM. Anzurstobart binds SIRPα at a CD47-overlapping site, blocks CD47-SIRPα interactions, inhibits CD47-SIRPα axis signaling, and binds across 6 prevalent human SIRPα haplotypes. Anzurstobart binds SIRPγ and inhibits CD47-SIRPγ interactions. Anzurstobart can be used for the research of non-Hodgkin's lymphoma, colorectal cancer, squamous cell carcinoma of the head and neck, diffuse large B-cell lymphoma, and advanced solid and hematologic malignancies^[1][2].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Human

SIRPa/CD172a

Anzurstobart (CC-95251) potently blocks CD47-SIRPα binding in a dose-dependent manner, with near-complete inhibition at 100 nM^[1].
Anzurstobart (50 nM; 180 seconds) demonstrates strong binding coverage across the six most prevalent human SIRPα haplotypes^[1].
Anzurstobart (20 nmol/L; 10 minutes preincubation, 3-hour coculture) alone dose-dependently increases macrophage-mediated phagocytosis of GP2d, GP5d, and SW480 colorectal cancer cells^[1].
Anzurstobart (20 nmol/L; 10 minutes preincubation, 3-hour coculture) in combination with Rituximab (HY-P9913) dose-dependently enhances macrophage-mediated phagocytosis of OCI-Ly3, RIVA, Pfeiffer, and Karpas 422 DLBCL cells, while Anzurstobart alone has limited phagocytic activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Anzurstobart (CC-95251) (10-100 mg/kg; i.v.; single dose, repeat dose) results in dose-dependent peak serum concentrations, a half-life of 163-227 hours, and no hematologic cell depletion over 28 days in Macaca fascicularis^[1].
Anzurstobart (10-100 mg/kg; i.v.) is well-tolerated in healthy cynomolgus monkeys with no hematologic depletion observed^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

140885  [NCBI]

P78324

ELISA, FACS, Functional assay

Unconjugated

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

144.66 kDa

2543693-10-1

Liquid

Colorless to light yellow

[Anzurstobart]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  Human IgG1 kappa

• 
  Flow Cytometry analysis of U937 cells labelling SIRPa/CD172a (red) with Anzurstobart (anti-SIRPa/CD172a) (HY-P990033). Goat Anti-Human IgG (Alexa Fluor 488) (HY-P83776) at a dilution of 1/1000 was used as the secondary antibody. Blue-Human IgG1 kappa (HY-P99001). Black-Unlabelled control, cells without incubation with primary antibody.

• [1]. Chan H, et al. Discovery and Preclinical Activity of BMS-986351, an Antibody to SIRPα That Enhances Macrophage-mediated Tumor Phagocytosis When Combined with Opsonizing Antibodies. Cancer Res Commun. 2024;4(2):505-515.  [Content Brief]

  [2]. Chan H, et al. Discovery and Preclinical Characterization of CC-95251, an Anti-SIRPα Antibody That Enhances Macrophage-Mediated Phagocytosis of Non-Hodgkin Lymphoma (NHL) Cells When Combined with Rituximab. Blood. 2021;2271-2272.