1088715-84-7
1088715-84-7 structure
- Name: LY2510924
- Chemical Name: LY2510924
- CAS Number: 1088715-84-7
- Molecular Formula: C62H88N14O10
- Molecular Weight: 1189.450
- Catalog: Signaling Pathways GPCR/G Protein CXCR
- Create Date: 2018-06-26 08:36:00
- Modify Date: 2024-01-09 12:23:02
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LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
| Name | LY2510924 |
|---|---|
| Synonyms |
1,4,7,10,13,16,19-Heptaazacyclotricosane-20-carboxamide, N-[(1S)-1-(aminocarbonyl)-5-[(1-methylethyl)amino]pentyl]-11-[3-[(aminoiminomethyl)amino]propyl]-5-[(4-hydroxyphenyl)methyl]-8-[4-[(1-methylethyl)amino]butyl]-14-(2-naphthalenylmethyl)-3,6,9,12,15,18,23-heptaoxo-2-(phenylmethyl)-, (2S,5S,8S,11R,14S,20R)-
(2S,5S,8S,11R,14S,20R)-N-[(2S)-1-Amino-6-(isopropylamino)-1-oxo-2-hexanyl]-2-benzyl-11-(3-carbamimidamidopropyl)-5-(4-hydroxybenzyl)-8-[4-(isopropylamino)butyl]-14-(2-naphthylmethyl)-3,6,9,12,15,18,23-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosane-20-carboxamide |
| Description | LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. |
|---|---|
| Related Catalog | |
| Target |
SDF-1α-CXCR4:79.7 pM (IC50) SDF-1α-CXCR4:49.5 pM (Ki) |
| In Vitro | 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]. |
| 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]. |
| Kinase Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C62H88N14O10 |
| Molecular Weight | 1189.450 |
| Exact Mass | 1188.680786 |
| LogP | 0.58 |
| Index of Refraction | 1.641 |
| Storage condition | 2-8℃ |