1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

LY2510924 

Cat. No.: HY-12488 Purity: >98.0%
Handling Instructions

LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.

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

LY2510924 Chemical Structure

LY2510924 Chemical Structure

CAS No. : 1088715-84-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 942 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
25 mg USD 1440 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 2280 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 3480 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.

IC50 & Target

IC50: 0.079 nM (SDF-1 binding to CXCR4)[1]

In Vitro

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].

In Vivo

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 0.8407 mL 4.2036 mL 8.4072 mL
5 mM 0.1681 mL 0.8407 mL 1.6814 mL
10 mM 0.0841 mL 0.4204 mL 0.8407 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

LY2510924 formulated in 1×PBS.

Mice: SCID female mice are injected intravenously with MDA-MB-231 cells, and are treated subcutaneously with vehicle (1×PBS) or 3 mg/kg of LY2510924 formulated in 1×PBS. Group 1 and 2 animals receive vehicle or 3 mg/kg of LY2510924 twice daily for days with treatment beginning on one day before tumor cell injection. Group 3 animals receive 3 mg/kg of LY2510924 15 twice daily for 13 days with treatment beginning one day after tumor cell injection. After treatment, lung tissues are fixed in 10% neutral-buffered formalin for at least 24 hours and lung lobes are present in histologic sections[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1189.45

Formula

C₆₂H₈₈N₁₄O₁₀

CAS No.

1088715-84-7

SMILES

O=C(NCC(N[[email protected]](CCC(N[[email protected]]1CC2=CC=CC=C2)=O)C(N[[email protected]](C(N)=O)CCCCNC(C)C)=O)=O)[[email protected]@H](NC([[email protected]@](NC([[email protected]@H](NC([[email protected]](NC1=O)CC3=CC=C(O)C=C3)=O)CCCCNC(C)C)=O)([H])CCCNC(N)=N)=O)CC4=CC(C=CC=C5)=C5C=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥125 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
LY2510924
Cat. No.:
HY-12488
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