| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CXCR4
MSX-130 targets CXCR4 (C-X-C chemokine receptor type 4), a seven-transmembrane G protein-coupled receptor (GPCR) belonging to the rhodopsin-like GPCR family. CXCR4 is the receptor for the chemokine CXCL12 (SDF-1) and plays a critical role in immune cell trafficking, hematopoiesis, and tissue development. By antagonizing CXCR4, MSX-130 blocks CXCL12-mediated signaling. |
|---|---|
| ln Vitro |
Members of the rhodopsin-like GPCR family, also known as family I GPCRs, include the seven transmembrane C-X-C chemokine receptor-4 (CXCR4) GPCR. In addition to regulating stem cell trafficking, CXCR4 is crucial for neovascularization and cancer metastasis [1].
In vitro, MSX-130 acts as a CXCR4 antagonist. It inhibits cancer cell migration and invasion by blocking CXCR4 signaling. CXCR4 is known to play a role in cancer metastasis. The compound's activity has been characterized in receptor binding and functional assays. |
| ln Vivo |
In vivo, MSX-130 inhibits tumor metastasis. It has been used in preclinical studies to investigate the role of CXCR4 in cancer progression and metastasis. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic profile.
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| Enzyme Assay |
In vitro receptor binding assays for MSX-130 typically use membrane preparations from cells expressing CXCR4. Radioligand binding is performed using [¹²⁵I]-CXCL12 or other CXCR4 radioligands. Membranes are incubated with radioligand and varying concentrations of MSX-130 in assay buffer. Nonspecific binding is determined using excess unlabeled ligand. Bound radioactivity is measured by filtration and scintillation counting. IC₅₀ and Ki values are calculated from competition curves. Functional assays measure CXCL12-induced calcium mobilization or chemotaxis.
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| Cell Assay |
For cell-based assays, cancer cell lines expressing CXCR4 are cultured in appropriate media. Cells are seeded in multi-well plates and treated with MSX-130 at various concentrations. Cell migration and invasion are assessed using Transwell or wound-healing assays. CXCR4 signaling is assessed by measuring downstream signaling events. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, MSX-130 may be administered to rodents for efficacy studies in cancer metastasis models. The compound is formulated in a suitable vehicle. Endpoints include tumor growth, metastasis assessment, and survival analysis.
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| ADME/Pharmacokinetics |
MSX-130 (MW 514.62, C₃₆H₂₆N₄) is a CXCR4 antagonist. It is slightly soluble in DMSO and DMF. Purity: ≥98%. Storage: -20°C. Detailed pharmacokinetic parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
MSX-130 is for research use only and is not intended for human therapeutic applications. Toxicity data are limited. Standard safety pharmacology and toxicology studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
MSX-130 is a research-grade CXCR4 antagonist for studying cancer metastasis and CXCR4 biology. Its primary applications include cancer research, immunology, and drug discovery. The compound is not an approved drug and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only.
|
| Molecular Formula |
C36H26N4
|
|---|---|
| Molecular Weight |
514.61844
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| Exact Mass |
514.215
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| Elemental Analysis |
C, 84.02; H, 5.09; N, 10.89
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| CAS # |
4051-59-6
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| PubChem CID |
4547410
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| Appearance |
Off-white to Pale Yellow Solid Powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
766.3±48.0 °C at 760 mmHg
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| Flash Point |
326.5±22.5 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
11.84
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
691
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=C(N=C(N2)C3=CC=C(C=C3)C4=NC(=C(N4)C5=CC=CC=C5)C6=CC=CC=C6)C7=CC=CC=C7
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| InChi Key |
MKRQQXYFSWSAIS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H26N4/c1-5-13-25(14-6-1)31-32(26-15-7-2-8-16-26)38-35(37-31)29-21-23-30(24-22-29)36-39-33(27-17-9-3-10-18-27)34(40-36)28-19-11-4-12-20-28/h1-24H,(H,37,38)(H,39,40)
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| Chemical Name |
2-[4-(4,5-diphenyl-1H-imidazol-2-yl)phenyl]-4,5-diphenyl-1H-imidazole
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| Synonyms |
MSX 130; MSX-130; MSX130
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 2~3 mg/mL (3.9~5.8 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9432 mL | 9.7159 mL | 19.4318 mL | |
| 5 mM | 0.3886 mL | 1.9432 mL | 3.8864 mL | |
| 10 mM | 0.1943 mL | 0.9716 mL | 1.9432 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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