2. Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. P2X Receptor FAK MMP
  4. P2X7R antagonist-1

P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research.

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P2X7R antagonist-1

P2X7R antagonist-1 Chemical Structure

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P2X7R antagonist-1 Related Antibodies

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Description

P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research[1].

IC50 & Target[1]

hP2X7R

3.57 μM (IC50)

MMP-9

 

In Vitro

P2X7R antagonist-1 (Compound 17d) (3.57-50 μM) potently inhibits the formation of P2X7R macropores in HEK293T-hP2X7R cells, with an IC50 value of 3.57 μM[1].
P2X7R antagonist-1 reduces the inhibitory activity against topoisomerase II (IC50 = 9.23 μM) and improves the target selectivity for P2X7R[1].
P2X7R antagonist-1 (5 μM) exhibits broad-spectrum antiproliferative activity in MCF-7, HGC-27, MKN-45, TE-1, KYSE-150, 4T1 and B16-F10 cells, with relatively strong activity in MCF-7 cells (IC50 = 0.42 μM). The inhibition rates at 5 μM are 96.3%, 92.7%, 84.7%, 90.8%, 86.5%, 86.1% and 44.3%, respectively[1].
P2X7R antagonist-1 (50-200 nM) inhibits the invasion and migration of human breast cancer MCF-7 cells in a dose-dependent manner by downregulating the expression of FAK and MMP-9[1].
P2X7R antagonist-1 (17d) (0.1 μM) exhibits antimetastatic activity against human breast cancer MCF-7 cells, which is mainly mediated by the inhibition of P2X7R; this is confirmed by the reduced potency observed in P2X7R-knockdown cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

P2X7R antagonist-1 Related Antibodies

Cell Migration Assay [1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 50, 100, 200 nM
Incubation Time: 48 h
Result: Inhibited invasion and migration.
Parmacokinetics
Species Dose Route Cmax T1/2 Tmax AUClast CL F
Rat[1] 5 mg/kg i.v. / 2.62 h / 34588 ng·h/mL 46.41 mL/min/kg /
Rat[1] 20 mg/kg p.o. 48498 ng/mL 3.91 h 0.83 h 52109 ng/L.h 72.68 mL/min/kg 37.6 %
In Vivo

P2X7R antagonist-1 (5-20 mg/kg, i.p., administered once every 2 to 3 days for 19 days) dose-dependently inhibits the growth and metastasis of PD-1-resistant breast cancer in female BALB/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (6-8 weeks) (4T1 cells, 3×107/mL)[1]
Dosage: 5, 10, 20 mg/kg
Administration: i.p., every 2-3 day, 19 days
Result: Inhibited the growth and metastasis of PD-1-resistant breast cancer in female BALB/c mice, while enhancing the infiltration and activation of CD4+ and CD8+ T cells in the tumor microenvironment, with no systemic toxicity observed.
Molecular Weight

453.53

Formula

C24H31N5O4
SMILES

CC(NCCNC1=CC=C(C2=C1C(C3=CC=CC([N+]([O-])=O)=C3C2=O)=O)NCCNC(C)C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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P2X7R antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

P2X7R antagonist-1P2X ReceptorFAKMMPP2XRsPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseMatrix metalloproteinasesMCF-7 human breast cancer cellsP2X7 receptorCD4 T cellanti-PD-1 monoclonal antibodiesfemale BALB/c miceHEK293T-hP2X7R cellsPD-1-resistant breast cancermurine breast cancer modelsbreast cancerCD8 T cellInhibitorinhibitorinhibit

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