Anzurstobart
Based on 1 Customer Validation
Anzurstobart (CC-95251; BMS-986351) is a CD47/SIRPα inhibitor with human SIRPα Kd 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.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 2543693-10-1
- Molecular Weight:144.66 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Isotype
Human IgG1 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
SIRPa/CD172a
In Vitro
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. Further protocols information, click here.
Parmacokinetics
In Vivo
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.
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Animal Model:Cynomolgus monkeys[2]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:i.v.; single dose (day 1); repeat dose (day 15)
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Result:Reached peak serum concentrations (Cmax) of 183 μg/mL (10 mg/kg), 632 μg/mL (30 mg/kg), and 1984 μg/mL (100 mg/kg) after day 1 dose.
Reached peak serum concentrations (Cmax) of 183 μg/mL (10 mg/kg), 664 μg/mL (30 mg/kg), and 2276 μg/mL (100 mg/kg) after day 15 dose.
Exhibited half-life (T1/2) ranging from 163 to 227 hours across individual animals.
Showed clearance rates ranging from 7.77 to 15.48 mL/day/kg.
Caused no depletion of white blood cells, monocytes, lymphocytes, or red blood cells over 28 days of exposure.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG1 kappa
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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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.
Chemical Information
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CAS No. 2543693-10-1
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Appearance Liquid
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Molecular Weight 144.66 kDa
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Color Colorless to light yellow
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SMILES
[Anzurstobart]
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Synonyms
CC-95251; BMS-986351
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)