MSX-122
Based on 1 publication(s) in Google Scholar
MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.
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- Pureté: 98.16%
- CAS No.: 897657-95-3
- Formule: C16H16N6
- Masse moléculaire:292.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) MSX-122
More
Activité biologique
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CXCR4/CXCL12 ~10 nM (IC50) |
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 shows no inhibition on cAMP reduction mediated by their corresponding ligands CCR3/CCL5 and CCR5/CCL5. MSX-122 (100 nM) potently blocks invasion of 78% MDA-MB-231 cells. However, MSX-122 does not suppress T-tropic HIV infection and is inactive in calcium flux assay[1].
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 897657-95-3
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Appearance Solid
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Masse moléculaire 292.34
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Formule C16H16N6
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Color Light yellow to yellow
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SMILES
C1(CNC2=NC=CC=N2)=CC=C(CNC3=NC=CC=N3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Br J Haematol
CXCR4 antagonists disrupt leukaemia-meningeal cell adhesion and attenuate chemoresistance. [Abstract]2023 May;201(3):459-469. PMID: 36535585
Solvant et solubilité
DMSO : 4 mg/mL (13.68 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 0.4 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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: ≥ 0.4 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (34.21 mM); Suspended solution; Need ultrasonic
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.
Protocole
Mice[1]
Six- to eight-week-old female nude mice are given injections of 1.5×106 MDA-MB-231 breast cancer cells mixed with the compound (1 µM, less than 5 min preincubation) through the tail vein (10/group). From the following day, mice in the treated group are given 4 mg/kg MSX-122ms (salt form) daily by i.p. injection. The animals are sacrificed 35 days after the tumor cell injection. Whole lung tissues are harvested and sectioned for real-time RT-PCR for human CXCR4 and H&E histostaining to evaluate the metastatic tumor area in five fields per section microscopically. These experiments are repeated once more to confirm the results. For the head and neck cancer animal model, metastatic subclones of 686LN-Ms cells are injected in the same way as MDA-MB-231 cells. [18F]FDG-PET is performed. For the uveal melanoma micrometastasis mouse model, on day 0, each mouse is inoculated with 1×106 wild-type OMM2.3 cells expressing HGF/TGF-β/CXCR4/MMP2 into the posterior chamber of right eye. On day 3, mice are treated with 10 mg/kg MSX-122 in 0.1 mL volume of 45% CD daily by i.p. injection, whereas the control mice are injected with 0.1 mL 45% CD only. On day 7, eyes with tumor are enucleated. The growth of tumor is checked by histological methods. On day 28, hepatic tissues are collected and fixed in 10% formalin, processed, H&E stained, and the number of hepatic micrometastases is counted under microscope. Six sections through the center of the liver are microscopically examined for the presence of micrometastases (<100 µm diameter) and the average number of micrometastases per section is determined. Ten mice per group are used. A table summarizing animal experiments for three metastasis models can be found in the Data S3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4207 mL | 17.1034 mL | 34.2067 mL | 85.5169 mL |
| 5 mM | 0.6841 mL | 3.4207 mL | 6.8413 mL | 17.1034 mL | |
| 10 mM | 0.3421 mL | 1.7103 mL | 3.4207 mL | 8.5517 mL |
MSX-122 Related Classifications
HY-13696 Related Classifications
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