LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM. LY2510924 inhibits SDF-1-induced cell migration (IC50 = 0.26 nM) in human lymphoma U937 cells expressing endogenous CXCR4. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.
| Cell Experiment | |
|---|---|
| Cell lines | U937 cells |
| Preparation method | Briefly, U937 cells were harvested and washed once with chemotaxis assay buffer prepared with 1× RPMI medium containing 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. Cells were then resuspended in assay buffer at a density of 5 × 106 cells/mL. The assay was performed in a 96-well ChemoTx plate (NeuroProbe). Generally, 50 μL of cell mixture with or without LY2510924 was plated on the upper chamber, and 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer was added to the lower chamber. The plate was then incubated for 2.5 hours at 37°C. Following the incubation, 5 μL of CellTiter 96 AQ (Promega) was added into the lower chamber. The plate was then incubated for 60 minutes at 37°C. The migrated cells were detected by measuring the absorbance at 492 nm with a Tecan Spectrafluor Plus Microplate Reader. |
| Concentrations | 0-10 uM |
| Incubation time | 2.5 h |
| Animal Experiment | |
|---|---|
| Animal models | female C57/BL6 mice, male Sprague-Dawley rats, male Beagle dogs, and male Cynomolgus monkeys at fasted state |
| Formulation | formulated in 1× PBS |
| Dosages | 3 mg/kg |
| Administration | s.c. or i.v. |
| Molecular Weight | 1189.45 |
| Formula | C62H88N14O10 |
| CAS Number | 1088715-84-7 |
| Solubility (25°C) | Water 45 mg/mL DMSO 120 mg/mL |
| Storage | -20°C, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CXCR Products |
|---|
| FC131 TFA
FC131 TFA is a CXCR4 antagonist, inhibits [125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. |
| CTCE-0214
CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. |
| TC14012
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. |
| CXCR4 antagonist 4
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM). |
| Ac-Pro-Gly-Pro-OH
Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
