MEDI-3185
MEDI-3185 is a potent CXCR4 antagonist. MEDI-3185 binds CXCR4 via CDR3H and ECL2 β-strand/β-strand interaction, blocks SDF-1 access and displaces SDF-1. MEDI-3185 can be used for the research of hematologic tumors, ovarian tumors.
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Actividad biológica
Human
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CXCR4 |
MEDI-3185 (0.381 pM-200 nM; 5 h) binds to CXCR4 on cynomolgus monkey HSC-F cells with an on-cell Kd of 221.0 pM[1].
MEDI-3185 (1 hour) dose-dependently occupies CXCR4 on cynomolgus monkey CD3+ lymphocytes in vitro with an IC50 of 241.1 pM, with minimal assay displacement interference[1].
MEDI-3185 (12.5-50 μg/mL) does not cross-react with human CXCR7[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MEDI-3185 (15-150 mg/kg; i.v.; weekly; 13 weeks) maintains near-complete CXCR4 receptor occupancy with weekly dosing in cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Macaca fascicularis (male)[1]
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Dosage:0.01 mg/kg; 0.1 mg/kg; 1 mg/kg
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Administration:i.v.; single dose
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Result:Decreased free CXCR4 on CD3+ lymphocytes to 62% of predose values at 1 hour after 0.01 mg/kg dosing, with full recovery by 24 hours.
Showed total surface CXCR4 levels indistinguishable from vehicle control at 0.01 mg/kg.
Reached full free CXCR4 occupancy (~0.4% of baseline) on CD3+ lymphocytes at 1 hour after 0.1 mg/kg dosing, with full recovery by 24 hours.
Showed total surface CXCR4 levels indistinguishable from vehicle control at 0.1 mg/kg.
Maintained full free CXCR4 occupancy on CD3+ lymphocytes for 1 day after 1 mg/kg dosing, with gradual recovery by day 7.
Increased total CXCR4 on CD3+ lymphocytes to a maximum of 4.38-fold of baseline at 1 mg/kg.
Elevated surface CXCR4 on granulocytes, CD3+ lymphocytes, CD3- lymphocytes, and monocytes at 1 mg/kg, with the highest increase observed at 1 and 2 days after dosing.
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Animal Model:Macaca fascicularis (male, female)[1]
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Dosage:15 mg/kg; 50 mg/kg; 150 mg/kg
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Administration:i.v.; weekly; 13 weeks
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Result:Maintained group median free CXCR4 on CD3+ lymphocytes at less than 0.44% of baseline throughout the dosing period across all dose levels.
Observed paradoxical full free CXCR4 occupancy in ADA-positive animals at 15 mg/kg when MEDI-3185 was undetectable in serum, representing an assay artifact.
Increased total CXCR4 on CD3+ lymphocytes 9.1-fold after the first dose and maintained levels above 4.6-fold of baseline throughout the dosing period in ADA-negative animals dosed at 15 mg/kg.
Increased total CXCR4 on CD3+ lymphocytes 7.7-fold after the first dose, declined to 0.8-fold of baseline at Day 21, increased to 2.5-fold of baseline at Day 91, and returned to baseline by Day 119 in ADA-positive animals dosed at 15 mg/kg.
CXCR4/CD184
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Schwickart M, et al. Evaluation of assay interference and interpretation of CXCR4 receptor occupancy results in a preclinical study with MEDI3185, a fully human antibody to CXCR4. Cytometry B Clin Cytom. 2016;90(2):209-219. [Content Brief]
[2]. Peng L, et al. Molecular basis for the antagonistic activity of an anti-CXCR4 antibody. MAbs. 2016;8(1):163-175. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MEDI-3185 Related Classifications
HY-P992405 Related Classifications
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