| Identification | Back Directory | [Name]
Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2 | [CAS]
1088715-84-7 | [Synonyms]
CS-2675
LY2510924
LY2510924; LY-2510924; LY 2510924
Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2
Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2A
L-Lysinamide, L-phenylalanyl-L-tyrosyl-N6-(1-methylethyl)-L-lysyl-D-arginyl-3-(2-naphthalenyl)-L-alanylglycyl-D-α-glutamyl-N6-(1-methylethyl)-, (7→1)-lactam | [Molecular Formula]
C62H88N14O10 | [MDL Number]
MFCD31728513 | [MOL File]
1088715-84-7.mol | [Molecular Weight]
1189.45 |
| Chemical Properties | Back Directory | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 125 mg/mL (105.09 mM) | [form ]
Solid | [pka]
9.89±0.15(Predicted) | [color ]
White to off-white | [InChIKey]
IJHWVENTEFSNBC-QBSDWBABNA-N |
| Hazard Information | Back Directory | [Uses]
LY2510924 is a CXC chemokine receptor 4 inhibitor and a potential antineoplastic agent. | [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]. | [IC 50]
125I-SDF-1α-CXCR4: 79.7 pM (IC50); 125I-SDF-1α-CXCR4: 49.5 pM (Ki) | [storage]
Store at -20°C |
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