Home Immunology & Inflammation CXCR antagonist LY2510924

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LY2510924 CXCR antagonist

Cat.No.S8505

LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L.
LY2510924 CXCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 1189.45

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Quality Control

Batch: Purity: 99.84%
99.84

Solubility

In vitro
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Water : 100 mg/mL

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Chemical Information, Storage & Stability

Molecular Weight 1189.45 Formula

C62H88N14O10

 Storage (From the date of receipt)
CAS No. 1088715-84-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)NCCCCC1C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(CCC(=O)NC(C(=O)NC(C(=O)N1)CC2=CC=C(C=C2)O)CC3=CC=CC=C3)C(=O)NC(CCCCNC(C)C)C(=O)N)CC4=CC5=CC=CC=C5C=C4)CCCN=C(N)N

Mechanism of Action

Targets/IC50/Ki
CXCR4
(Cell-free)
0.079 nM
In vitro
In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1-induced cell migration with IC50 value of 0.26 nmol/L and inhibits SDF-1/CXCR4-mediated intracellular signaling. This compound exhibits a concentration-dependent inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveal that it has no apparent agonist activity. It has no inhibitory activities against other chemokine receptors including CCR1, CCR2, CXCR2, and CXCR3 at the concentrations tested. Similarly, there is no activity observed among serotonin, dopamine, and opioid receptors.
In vivo
LY2510924 has acceptable in vivo stability and a pharmacokinetic profile similar to a typical small-molecular inhibitor in preclinical species. This compound shows dose-dependent inhibition of tumor growth in human xenograft models developed with non-Hodgkin lymphoma, renal cell carcinoma, lung, and colon cancer cells that express functional CXCR4. In MDA-MB-231, a breast cancer metastatic model, it inhibits tumor metastasis by blocking migration/homing process of tumor cells to the lung and by inhibiting cell proliferation after tumor cell homing. This chemical has a dramatically improved in vivo stability with a half-life of 3 to 5 hours in preclinical species and 9.16 hours in humans at the recommended phase II dose.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02737072 Terminated
Solid Tumor
Eli Lilly and Company|AstraZeneca
 September 2016 Phase 1
NCT02652871 Completed
Leukemia
M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program
 May 9 2016 Phase 1

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