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CXCR4 antagonist 6
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Catalog No. T61420Cas No. 2304750-68-1
CXCR4 antagonist 6 (compound 46) is a highly potent small-molecule inhibitor of the chemokine receptor CXCR4 with an IC50 value of 79 nM, effectively suppressing CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, significantly inhibiting CXCL12/CXCR4-mediated cell migration, and demonstrating pronounced therapeutic efficacy in a mouse model of cancer metastasis, highlighting its value for cancer biology, metastasis research, and chemokine signaling studies.
CXCR4 antagonist 6
😃Good
Purity: 100%
Catalog No. T61420Cas No. 2304750-68-1
CXCR4 antagonist 6 (compound 46) is a highly potent small-molecule inhibitor of the chemokine receptor CXCR4 with an IC50 value of 79 nM, effectively suppressing CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, significantly inhibiting CXCL12/CXCR4-mediated cell migration, and demonstrating pronounced therapeutic efficacy in a mouse model of cancer metastasis, highlighting its value for cancer biology, metastasis research, and chemokine signaling studies.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $462 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:100%
ee:100%
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Product Introduction
Bioactivity
Chemical Properties
| Description | CXCR4 antagonist 6 (compound 46) is a highly potent small-molecule inhibitor of the chemokine receptor CXCR4 with an IC50 value of 79 nM, effectively suppressing CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, significantly inhibiting CXCL12/CXCR4-mediated cell migration, and demonstrating pronounced therapeutic efficacy in a mouse model of cancer metastasis, highlighting its value for cancer biology, metastasis research, and chemokine signaling studies. |
| Targets&IC50 | CXCR4:79 nM, CXCL12:0.12 nM |
| In vitro | Method: Novel CXCR4 antagonists based on a pyrrolidine scaffold were synthesized and evaluated using receptor binding assays, calcium flux assays, transwell migration assays, liver microsome stability tests, and a mouse cancer metastasis model. Result: CXCR4 antagonist 6 showed potent CXCR4 antagonism with IC₅₀ values of 79 nM for receptor binding and 0.25 nM for calcium flux inhibition, reduced CXCL12-mediated cell migration, exhibited improved metabolic stability, and demonstrated significant anti-metastatic efficacy in mice[1]. |
| Molecular Weight | 366.5 |
| Formula | C21H30N6 |
| Cas No. | 2304750-68-1 |
| Smiles | C(N1[C@@H](CCC1)C2=C(C)C=CC=N2)C=3C=C(N=C(C)N3)N4CCN(C)CC4 |
| Color | Yellow |
| Appearance | Oil |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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