LY2510924

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206068

CAS#: 1088715-84-7

Description: LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity. Upon subcutaneous administration, CXCR4 inhibitor LY2510924 binds to the chemokine receptor CXCR4, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor activation. This may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types.


Chemical Structure

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LY2510924
CAS# 1088715-84-7

Theoretical Analysis

MedKoo Cat#: 206068
Name: LY2510924
CAS#: 1088715-84-7
Chemical Formula: C62H87N13O11
Exact Mass: 1189.6648
Molecular Weight: 1190.458
Elemental Analysis: C, 62.55; H, 7.37; N, 15.30; O, 14.78

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Synonym: LY2510924; LY-2510924; LY 2510924, Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2

IUPAC/Chemical Name: (2S,5S,20R)-N-((S)-1-amino-6-(isopropylamino)-1-oxohexan-2-yl)-2-benzyl-5-(4-hydroxybenzyl)-8-(4-(isopropylamino)butyl)-14-(naphthalen-2-ylmethyl)-3,6,9,12,15,18,23-heptaoxo-11-(3-ureidopropyl)-1,4,7,10,13,16,19-heptaazacyclotricosane-20-carboxamide

InChi Key: DDZCMBOHPTXPRC-AOSPDLCISA-N

InChi Code: InChI=1S/C62H87N13O11/c1-38(2)65-30-12-10-19-46(55(63)79)71-59(83)49-28-29-53(77)70-51(34-40-15-6-5-7-16-40)60(84)75-52(35-41-23-26-45(76)27-24-41)61(85)73-47(20-11-13-31-66-39(3)4)57(81)72-48(21-14-32-67-62(64)86)58(82)74-50(56(80)68-37-54(78)69-49)36-42-22-25-43-17-8-9-18-44(43)33-42/h5-9,15-18,22-27,33,38-39,46-52,65-66,76H,10-14,19-21,28-32,34-37H2,1-4H3,(H2,63,79)(H,68,80)(H,69,78)(H,70,77)(H,71,83)(H,72,81)(H,73,85)(H,74,82)(H,75,84)(H3,64,67,86)/t46-,47?,48?,49+,50?,51-,52-/m0/s1

SMILES Code: 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

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 1190.458 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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 1: Cho BS, Zeng Z, Mu H, Wang Z, Konoplev S, McQueen T, Protopopova M, Cortes J,
Marszalek JR, Peng SB, Ma W, Davis RE, Thornton DE, Andreeff M, Konopleva M.
Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as
monotherapy and in combination with chemotherapy. Blood. 2015 Jul
9;126(2):222-32. doi: 10.1182/blood-2015-02-628677. Epub 2015 Jun 1. Erratum in:
Blood. 2015 Aug 20;126(8):1049. Konoplev, Sergej [added]. PubMed PMID: 26031918;
PubMed Central PMCID: PMC4497963.

2: Peng SB, Zhang X, Paul D, Kays LM, Gough W, Stewart J, Uhlik MT, Chen Q, Hui
YH, Zamek-Gliszczynski MJ, Wijsman JA, Credille KM, Yan LZ. Identification of
LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor
activities in solid tumor and breast cancer metastatic models. Mol Cancer Ther.
2015 Feb;14(2):480-90. doi: 10.1158/1535-7163.MCT-14-0850. Epub 2014 Dec 12.
PubMed PMID: 25504752.

3: Galsky MD, Vogelzang NJ, Conkling P, Raddad E, Polzer J, Roberson S, Stille
JR, Saleh M, Thornton D. A phase I trial of LY2510924, a CXCR4 peptide
antagonist, in patients with advanced cancer. Clin Cancer Res. 2014 Jul
1;20(13):3581-8. doi: 10.1158/1078-0432.CCR-13-2686. Epub 2014 Apr 11. Erratum
in: Clin Cancer Res. 2014 Aug 15;20(16):4414. PubMed PMID: 24727324.

(Last updated: 4/21/2016)



Additional Information