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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 |
| 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 | CXCL12:0.12 nM, CXCR4:79 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 |
| 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. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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