LY-2510924

Research use only, not for human use.

LY-2510924 (LY2510924)?is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM.

LY-2510924 (LY2510924)?is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity; inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling; exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells; shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.Kidney Cancer Phase 2 Clinical.

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. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.

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. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.

LY2510924

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Cancer

Kidney Cancer

1088715-84-7

1189.45

C62H88N14O10

>98% (HPLC)

DMSO : ≥ 125 mg/mL105.09 mM

O=C(NCC(N[C@@H](C(N[C@@H](CCCCNC(C)C)C(N)=O)=O)CCC(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC2=CC=C(O)C=C2)C3=O)=O)=O)=O)C(CC4=CC=C(C=CC=C5)C5=C4)NC(C(CCCNC(N)=O)NC(C(N3)CCCCNC(C)C)=O)=O

Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2

(-20℃)

With Ice Pack

≥ 2 years