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
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • 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[1]

SDF-1α-CXCR4

79.7 pM (IC50)

SDF-1α-CXCR4

49.5 pM (Ki)

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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (105.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
References
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]

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

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

Cat. No.: HY-12488