LY-2510924

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

Cat No.:V4853 Purity: ≥98%

COA Product Data Instructions for use SDS

LY2510924 (LY-2510924),a small cyclicpeptide, is a novel, potent and selective CXCR4 (CXC chemokine receptor 4) antagonist with potential anticancer and anti-inflammatory activity.

LY-2510924 Chemical Structure CAS No.: 1088715-84-7
Product category: CXCR

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

ADD TO CART CHECKOUT BULK INQUIRY

1-708-310-1919 sales@invivochem.com

Official Supplier of:

Business Relationship with 5000+ Clients Globally
Major Universities, Research Institutions, Biotech & Pharma
Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

LY2510924 (LY-2510924), a small cyclic peptide, is a novel, potent and selective CXCR4 (CXC chemokine receptor 4) antagonist with potential anticancer and anti-inflammatory activity. It inhibits SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. LY2510924 may have antitumor effects since it inhibits the CXC chemokine receptor 4 (CXCR4). Upon subcutaneous administration, the CXCR4 inhibitor LY2510924 binds to the chemokine receptor CXCR4, preventing CXCR4 from binding to its ligand, stromal derived factor-1 (SDF-1), and consequent receptor activation. Tumor cell migration and proliferation may be reduced as a result of this. Chemokine receptor CXCR4, which is part of the G protein-coupled receptor (GPCR) gene family, is upregulated in various tumor cell types and is involved in angiogenesis and chemotaxis.

Biological Activity I Assay Protocols (From Reference)

Targets

¹²⁵I-SDF-1α-CXCR4 ( Ki = 79.7 pM ); ¹²⁵I-SDF-1α-CXCR4 ( Ki = 49.5 pM )

ln Vitro

LY2510924 selectively inhibits SDF-1-induced GTP binding with a Kb value of 0.38 nM and blocks SDF-1 binding to CXCR4 with an IC50 value of 0.079 nM. LY2510924 inhibits SDF-1-induced cell migration and SDF-1/CXCR4-mediated intracellular signaling in human lymphoma U937 cells that express endogenous CXCR4. The IC50 value of this inhibitor is 0.26 nM. Tumor cells stimulated with SDF-1 show concentration-dependent inhibition of phospho-ERK and phospho-Akt. LY2510924 does not appear to have any agonist activity, according to biochemical and cellular analyses[1]. The main effects of LY2510924 are to reduce stromal cell defense against chemotherapy and to inhibit AML cell proliferation with minimal induction of cell death[2].

ln Vivo

Enzyme Assay

Cell Assay

After harvesting U937 cells, they are gently rinsed once with chemotaxis assay buffer, which is made with 1× RPMI medium that contains 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. At a density of 5 × 10⁶ cells/mL, the cells are then resuspended in assay buffer. A 96-well ChemoTx plate is used for the assay. Usually, the lower chamber was filled with 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer, while the upper chamber was plated with 50 μL of cell mixture, either with or without LY2510924. The plate is then incubated at 37°C for 2.5 hours. After the incubation period, the lower chamber is filled with 5 μL of CellTiter 96 AQ. The plate is then incubated at 37°C for 60 minutes. By measuring the absorbance at 492 nm, the migrated cells can be identified.

Animal Protocol

Mice: MDA-MB-231 cells are injected intravenously into female SCID mice, and they receive subcutaneous injections of either vehicle (1×PBS) or LY2510924 (3 mg/kg) formulated in 1×PBS. The animals in Groups 1 and 2 are treated with either a vehicle or 3 mg/kg of LY2510924 twice a day for several days, starting one day prior to the injection of tumor cells. Treatment for Group 3 animals starts one day after tumor cell injection and lasts for 13 days, with each animal receiving 3 mg/kg of LY2510924 15 twice daily. Lung lobes are visible in histologic sections after lung tissues are preserved in 10% neutral-buffered formalin for at least 24 hours following treatment[1].

References

[1]. 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.

[2]. Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as monotherapy and in combination with chemotherapy. Blood. 2015 Jul 9;126(2):222-32.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C62H88N14O10
Molecular Weight	1189.45
Exact Mass	1189.66
Elemental Analysis	C, 62.55; H, 7.37; N, 15.30; O, 14.78
CAS #	1088715-84-7
Appearance	Solid powder
SMILES	CC(C)NCCCC[C@H]1C(=O)N[C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](CCC(=O)N[C@H](C(=O)N[C@@H](C(=O)N1)CC2=CC=C(C=C2)O)CC3=CC=CC=C3)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N)CC4=CC5=CC=CC=C5C=C4)CCCN=C(N)N
InChi Key	IJHWVENTEFSNBC-OFPUNPKKSA-N
InChi Code	InChI=1S/C62H88N14O10/c1-38(2)66-30-12-10-19-46(55(63)80)72-59(84)49-28-29-53(78)71-51(34-40-15-6-5-7-16-40)60(85)76-52(35-41-23-26-45(77)27-24-41)61(86)74-47(20-11-13-31-67-39(3)4)57(82)73-48(21-14-32-68-62(64)65)58(83)75-50(56(81)69-37-54(79)70-49)36-42-22-25-43-17-8-9-18-44(43)33-42/h5-9,15-18,22-27,33,38-39,46-52,66-67,77H,10-14,19-21,28-32,34-37H2,1-4H3,(H2,63,80)(H,69,81)(H,70,79)(H,71,78)(H,72,84)(H,73,82)(H,74,86)(H,75,83)(H,76,85)(H4,64,65,68)/t46-,47-,48+,49+,50-,51-,52+/m0/s1
Chemical Name	(2S,5R,8S,11R,14S,20R)-N-[(2S)-1-amino-1-oxo-6-(propan-2-ylamino)hexan-2-yl]-2-benzyl-11-[3-(diaminomethylideneamino)propyl]-5-[(4-hydroxyphenyl)methyl]-14-(naphthalen-2-ylmethyl)-3,6,9,12,15,18,23-heptaoxo-8-[4-(propan-2-ylamino)butyl]-1,4,7,10,13,16,19-heptazacyclotricosane-20-carboxamide
Synonyms	LY2510924; LY-2510924; LY 2510924; Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ≥ 125 mg/mL (~105.1 mM) Water: ~100 mg/mL
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ≥ 125 mg/mL (~105.1 mM)
Water: ~100 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (1.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculate Reset

Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02652871	Completed	Drug: LY2510924 Drug: Idarubicin Drug: Cytarabine	Leukemia	M.D. Anderson Cancer Center	May 9, 2016	Phase 1
NCT01439568	Completed	Drug: LY2510924 Drug: Etoposide Drug: Carboplatin	Extensive Stage Small Cell Lung Carcinoma	Eli Lilly and Company	September 2011	Phase 2

Biological Data

LY2510924 rapidly and durably blocks surface CXCR4 and inhibits SDF-1α–induced chemotaxis and prosurvival signals of leukemic cells. Blood . 2015 Jul 9;126(2):222-32.
LY2510924 inhibits proliferation of AML cells and reverses stroma-mediated chemoresistance. Blood . 2015 Jul 9;126(2):222-32.
LY2510924 monotherapy has antileukemia activity in OCI-AML3 xenograft models. Blood . 2015 Jul 9;126(2):222-32.