EMU-116
Based on 1 Customer Validation
EMU-116 is an orally active CXCR4 antagonist. EMU-116 blocks the CXCL12-CXCR4 signaling axis by competitively binding to the CXCR4 receptor, thereby achieving broad mobilization of bone marrow stem/progenitor cells and immune cells into peripheral blood while simultaneously inhibiting tumor metastasis and microenvironmental immunosuppression. EMU-116 can be used for research on cancer, chemotherapy-induced neutropenia, and sickle cell disease.
For research use only. We do not sell to patients.
- Purity : 98.53%
- CAS No.: 2241724-59-2
- Formula: C25H35N5
- Molecular Weight:405.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CXCR4/CXCL12 |
In Vivo
EMU-116 (30 mg/kg; p.o.; once daily; administered from day 5 for a total of 8 days) significantly accelerates hematopoietic recovery of bone marrow stem cells in the Cyclophosphamide (HY-17420)-pretreatment-induced neutropenia model in Swiss mice, causing white blood cell, neutrophil, lymphocyte, and monocyte counts to rebound 3 days earlier than those of the control group[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA mice[3]
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Dosage:10 mg/kg (s.c.); 30 mg/kg (p.o.)
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Administration:s.c. or p.o.; single dose
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Result:Produced robust and sustained increases in WBCs, neutrophils, T-cells, and LSK+ cells, and these responses were superior to Plerixafor.
Responses tended to peak around 6 hours.
Induced pan-mobilization of mature hematopoietic subsets, with fold changes from baseline ranging from 40-fold for pDCs to 2-fold for eosinophils.
LSK and CFU counts correlated well.
No changes compared with vehicle control were observed in RBC indices, including RBC number, HCT, MCV, MCH, and Hb.
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Animal Model:Swiss mice[3]
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Dosage:30 mg/kg
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Administration:p.o.; once daily; 8 days
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Result:Mice rebounded in WBCs, neutrophils, lymphocytes, and monocytes 3 days earlier than control groups.
Increases in HSCs were also observed earlier, indicating faster bone marrow recovery.
Responses were 5- to 20-fold above baseline and sustainable, with the height and downward return occurring within a 3-day period.
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Animal Model:Townes (6 sickle cell mice; 3 male, 3 female)[3]
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Dosage:4 mg/kg (s.c.); 30 mg/kg (p.o.)
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Administration:s.c. or p.o.; single dose; 6 h
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Result:Both s.c. and oral dosing mobilized multiple cell types, including WBCs and LSK cells.
Both routes mobilized more LSK cells than Plerixafor without the enhanced leukocytosis observed with Plerixafor.
Chemical Information
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CAS No. 2241724-59-2
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Appearance Solid
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Molecular Weight 405.58
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Formula C25H35N5
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Color Light yellow to yellow
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SMILES
CN1CCN(C2=CC=CC3=C2C[C@H](CN(C)[C@H]4CCCC5=C4N=CC=C5)NC3)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (246.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 5 mg/mL (12.33 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (12.33 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 1 mM | 2.4656 mL | 12.3280 mL | 24.6560 mL | 61.6401 mL |
| 5 mM | 0.4931 mL | 2.4656 mL | 4.9312 mL | 12.3280 mL | |
| 10 mM | 0.2466 mL | 1.2328 mL | 2.4656 mL | 6.1640 mL | |
| 15 mM | 0.1644 mL | 0.8219 mL | 1.6437 mL | 4.1093 mL | |
| 20 mM | 0.1233 mL | 0.6164 mL | 1.2328 mL | 3.0820 mL | |
| 25 mM | 0.0986 mL | 0.4931 mL | 0.9862 mL | 2.4656 mL | |
| 30 mM | 0.0822 mL | 0.4109 mL | 0.8219 mL | 2.0547 mL | |
| 40 mM | 0.0616 mL | 0.3082 mL | 0.6164 mL | 1.5410 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4931 mL | 1.2328 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4109 mL | 1.0273 mL | |
| 80 mM | 0.0308 mL | 0.1541 mL | 0.3082 mL | 0.7705 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6164 mL |
EMU-116 Related Classifications
HY-168531 Related Classifications
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