2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. 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.

For research use only. We do not sell to patients.

MEDI-3185

MEDI-3185 Chemical Structure

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MEDI-3185 Related Antibodies

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Description

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[2].

Species Reactivity

Human
IC50 & Target[1]

CXCR4

 

In Vitro

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 Related Antibodies
In Vivo

MEDI-3185 (0.01-1 mg/kg; i.v.; single dose) induces dose-dependent CXCR4 receptor occupancy and, at the highest single dose of 1 mg/kg, upregulates total CXCR4 surface expression across multiple circulating blood cell populations in cynomolgus monkeys[1].
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.

Animal Model: Macaca fascicularis (male)[1]
Dosage: 0.01 mg/kg; 0.1 mg/kg; 1 mg/kg
Administration: i.v.; single dose
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.
Animal Model: Macaca fascicularis (male, female)[1]
Dosage: 15 mg/kg; 50 mg/kg; 150 mg/kg
Administration: i.v.; weekly; 13 weeks
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.
Gene ID

7852  [NCBI]

Accession
Target

CXCR4/CD184
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

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

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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MEDI-3185 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MEDI-3185MEDI3185MEDI 3185CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsovarian tumorsCD3- lymphocytesmonocytesT-cellsCD3+ lymphocytesgranulocytesCXCR4SDF-1CXCR7hematologic tumorsInhibitorinhibitorinhibit

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