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LY2510924

Cat. No. M10230
LY2510924 Structure
Synonym:

LY-2510924

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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM. LY2510924 inhibits SDF-1-induced cell migration (IC50 = 0.26 nM) in human lymphoma U937 cells expressing endogenous CXCR4. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.

Protocol
Cell Experiment
Cell lines U937 cells
Preparation method Briefly, U937 cells were harvested and washed once with chemotaxis assay buffer prepared with 1× RPMI medium containing 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. Cells were then resuspended in assay buffer at a density of 5 × 106 cells/mL. The assay was performed in a 96-well ChemoTx plate (NeuroProbe). Generally, 50 μL of cell mixture with or without LY2510924 was plated on the upper chamber, and 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer was added to the lower chamber. The plate was then incubated for 2.5 hours at 37°C. Following the incubation, 5 μL of CellTiter 96 AQ (Promega) was added into the lower chamber. The plate was then incubated for 60 minutes at 37°C. The migrated cells were detected by measuring the absorbance at 492 nm with a Tecan Spectrafluor Plus Microplate Reader.
Concentrations 0-10 uM
Incubation time 2.5 h
Animal Experiment
Animal models female C57/BL6 mice, male Sprague-Dawley rats, male Beagle dogs, and male Cynomolgus monkeys at fasted state
Formulation formulated in 1× PBS
Dosages 3 mg/kg
Administration s.c. or i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 1189.45
Formula C62H88N14O10
CAS Number 1088715-84-7
Purity >99%
Solubility Water 45 mg/mL
DMSO 120 mg/mL
Storage -20°C, sealed
References

Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as monotherapy and in combination with chemotherapy
Byung-Sik Cho, et al. Blood. 2015 Jul 9;126(2):222-32. PMID: 26031918.

Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor and breast cancer metastatic models
Sheng-Bin Peng, et al. Mol Cancer Ther. 2015 Feb;14(2):480-90. PMID: 25504752.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2510924, LY-2510924 supplier, CXCR, inhibitors

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