Basic information Safety Supplier Related

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

Basic information Safety Supplier Related

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

Product Name:
Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2
Synonyms:
  • Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2
  • LY2510924
  • LY2510924; LY-2510924; LY 2510924
  • CS-2675
  • 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
  • (2S,5S,8S,11R,14S,20R)-N-((S)-1-Amino-6-(isopropylamino)-1-oxohexan-2-yl)-2-benzyl-11-(3-guanidinopropyl)-5-(4-hydroxybenzyl)-8-(4-(isopropylamino)butyl)-14-(naphthalen-2-ylmethyl)-3,6,9,12,15,18,23-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosane-20-carboxamide
  • LY2510924 TFA salt
CAS:
1088715-84-7
MF:
C62H88N14O10
MW:
1189.47
Mol File:
1088715-84-7.mol
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Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2 Chemical Properties

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

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)

Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2Supplier

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