LY2510924
Based on 13 publication(s) in Google Scholar
LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.85%
- CAS. Nr.: 1088715-84-7
- Formel: C62H88N14O10
- Molecular Weight:1189.45
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Speicherung:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY2510924
More- Nat Commun. 2018 Jul 4;9(1):2612. [Abstract]
- J Control Release. 2021 Jan 10;329:524-537. [Abstract]
- J Nucl Med. 2026 Jan 29:jnumed.125.269933. [Abstract]
- Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):29144-29154. [Abstract]
- J Autoimmun. 2024 Feb:143:103171. [Abstract]
- Cancer Gene Ther. 2020 Feb;27(1-2):45-55. [Abstract]
- J Lipid Res. 2019 Dec;60(12):2020-2033. [Abstract]
- Sci Rep. 2019 Oct 25;9(1):15284. [Abstract]
- Mol Pharm. 2019 Nov 4;16(11):4688-4695. [Abstract]
- BMC Cancer. 2019 Nov 26;19(1):1142. [Abstract]
- Arab J Gastroenterol. 2024 Feb;25(1):28-36. [Abstract]
- Universität Würzburg . 2022 Oct.
- Patent. US20220273751A1.
Customer Validation & Images
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Cell Migration/Invasion Assay
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WB
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RT-PCR
Biologische Aktivität
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125I-SDF-1α-CXCR4 79.7 pM (IC50) |
125I-SDF-1α-CXCR4 49.5 pM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1088715-84-7
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Appearance Solid
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Molecular Weight 1189.45
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Formel C62H88N14O10
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Color White to off-white
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
2018 Jul 4;9(1):2612. PMID: 29973594 -
J Control Release
Manipulating immune system using nanoparticles for an effective cancer treatment: Combination of targeted therapy and checkpoint blockage miRNA. [Abstract]2021 Jan 10;329:524-537. PMID: 32971203 -
J Nucl Med
2026 Jan 29:jnumed.125.269933. PMID: 41611474 -
Proc Natl Acad Sci U S A
Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists. [Abstract]2020 Nov 17;117(46):29144-29154. PMID: 33148803 -
J Autoimmun
2024 Feb:143:103171. PMID: 38306953 -
Cancer Gene Ther
Use of polymeric CXCR4 inhibitors as siRNA delivery vehicles for the treatment of acute myeloid leukemia. [Abstract]2020 Feb;27(1-2):45-55. PMID: 31028289 -
J Lipid Res
CXCL12 promotes atherosclerosis by downregulating ABCA1 expression via the CXCR4/GSK3β/β-cateninT120/TCF21 pathway. [Abstract]2019 Dec;60(12):2020-2033. PMID: 31662443 -
Sci Rep
C-terminal-modified LY2510924: a versatile scaffold for targeting C-X-C chemokine receptor type 4. [Abstract]2019 Oct 25;9(1):15284. PMID: 31653903 -
Mol Pharm
[68Ga]Ga/[177Lu]Lu-BL01, a Novel Theranostic Pair for Targeting C-X-C Chemokine Receptor 4. [Abstract]2019 Nov 4;16(11):4688-4695. PMID: 31545614 -
BMC Cancer
β2AR-HIF-1α-CXCL12 signaling of osteoblasts activated by isoproterenol promotes migration and invasion of prostate cancer cells. [Abstract]2019 Nov 26;19(1):1142. PMID: 31771535
LY2510924 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Nov 26;19(1):1142. [Abstract]
Effect of LY2510924 (10 nM) on migration and invasion of prostate cancer cells induced by osteoblasts triggered by ISO.
LY2510924 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Nov 26;19(1):1142. [Abstract]
PC-3 and DU145 cells were treated with CM from MC3T3E1 and primary osteoblasts in response to ISO with or without LY2510924 (10 nM) for 24 h, and expression of E-cadherin and Vimentin were detected by Western blotting.
LY2510924 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Nov 26;19(1):1142. [Abstract]
EMT-related biomarkers expression of PC-3 and DU145 were detected by qRT-PCR treated with LY2510924 (10 nM).
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Arab J Gastroenterol
C-X-C motif chemokine receptor 4 inhibition promotes the effect of plantamajoside in hepatocellular carcinoma. [Abstract]2024 Feb;25(1):28-36. PMID: 38220479 -
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Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (84.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (84.07 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (1.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: SCID female mice are injected intravenously with MDA-MB-231 cells, and are treated subcutaneously with vehicle (1×PBS) or 3 mg/kg of LY2510924 formulated in 1×PBS. Group 1 and 2 animals receive vehicle or 3 mg/kg of LY2510924 twice daily for days with treatment beginning on one day before tumor cell injection. Group 3 animals receive 3 mg/kg of LY2510924 15 twice daily for 13 days with treatment beginning one day after tumor cell injection. After treatment, lung tissues are fixed in 10% neutral-buffered formalin for at least 24 hours and lung lobes are present in histologic sections[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Peng SB, et al. 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. [Content Brief]
[2]. Cho BS, et al. Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as monotherapy and in combination with chemotherapy. Blood. 2015 Jul 9;126(2):222-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 0.8407 mL | 4.2036 mL | 8.4072 mL | 21.0181 mL |
| 5 mM | 0.1681 mL | 0.8407 mL | 1.6814 mL | 4.2036 mL | |
| 10 mM | 0.0841 mL | 0.4204 mL | 0.8407 mL | 2.1018 mL | |
| 15 mM | 0.0560 mL | 0.2802 mL | 0.5605 mL | 1.4012 mL | |
| 20 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0509 mL | |
| 25 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8407 mL | |
| 30 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7006 mL | |
| 40 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5255 mL | |
| 50 mM | 0.0168 mL | 0.0841 mL | 0.1681 mL | 0.4204 mL | |
| 60 mM | 0.0140 mL | 0.0701 mL | 0.1401 mL | 0.3503 mL | |
| 80 mM | 0.0105 mL | 0.0525 mL | 0.1051 mL | 0.2627 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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