1. GPCR/G Protein Immunology/Inflammation Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR
  2. CXCR ERK Akt
  3. BPRCX807

BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma.

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BPRCX807

BPRCX807 Chemical Structure

CAS No. : 2236595-58-5

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Description

BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma[1].

IC50 & Target[1]

CXCR4

 

In Vitro

BPRCX 807 (1.5 h) exhibits an IC50 value of 40.4 nM against HEK293T cells[1].
BPRCX 807 shows an EC50 value of 48.1 nM in CCRF-CEM cells[1].
BPRCX 807 (10 μM, 24-72 h) significantly inhibits CXCL12-induced accelerated wound closure in HCA-1 cells[1].
BPRCX 807 (0.1-1 μM, 17.5 h) significantly reduces the number of migrating HCA-1 cells at a concentration of 1 μM[1].
BPRCX 807 (10-20 μM, 24-48 h) restrains the hypoxia-induced increases in mesenchymal marker expression and alleviates the hypoxia-induced decrease in epithelial markers in HCA-1 cells in a dose-dependent manner[1].
BPRCX 807 (5-20 μM, 24 h) significantly inhibits CXCL12-mediated ERK and Akt phosphorylation in HCA-1 and JHH-7 cells[1].

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

Cell Migration Assay [1]

Cell Line: HCA-1 cells
Concentration: 10 μM
Incubation Time: 0 h, 24 h, 48 h, 72 h
Result: Significantly inhibited CXCL12-induced accelerated wound closure in HCA-1 cells.

Real Time qPCR[1]

Cell Line: Hypoxia-induced HCA-1 cells
Concentration: 10 μM, 20 μM
Incubation Time: 24 h, 48 h
Result: Increased in mesenchymal marker expression (including Slug, Fibronectin, N-cadherin, Vimentin, FOXC2, Zeb1, and Zeb2).
Alleviated the hypoxia-induced decrease in epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5).
In Vivo

BPRCX 807 (15 mg/kg, s.c., once daily for 14 days) alone or in combination with Sorafenib (HY-10201) significantly inhibits tumor growth in mouse models of HCA-1 cell allogeneic and JHH-7 cell xenograft[1].
BPRCX 807 (15 mg/kg, s.c., once daily for 14 days), when used in combination with Anti-PD-1, can recruit T cells and synergistically inhibit tumor growth in mice with HCA-1 cell allogeneic transplantation[1].

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

Animal Model: HCA-1 or JHH-7 cells were orally implanted into the livers of 7-week-old C3H/HeNCrNarl mice and 9-week-old BALB/cAnN.Cg Foxnlnu/CrlNarl mice, respectively[1].
Dosage: 15 mg/kg
Administration: S.c., once daily for 14 days
Result: Significantly inhibited tumor growth when used alone.
The effect is strongest when used in combination with sorafenib.
Combined use significantly prolongs overall survival.
Reduced tumor-associated macrophage (TAM) infiltration (F4/80+ cells).
Reprogramed TAMs to the M1 phenotype (increased CD86+) and suppresses the M2 phenotype (decreased CD206+).
Increased cytotoxic CD8+ T cell infiltration.
Animal Model: HCA-1 cells were in situ implanted into 7-week-old C3H/HeNCrNarl mice. For combined anti-PD-1 immunotherapy, mice were intraperitoneally injected with anti-mouse PD-1 antibodies 10 days after tumor implantation[1].
Dosage: 15 mg/kg
Administration: S.c., once daily for 14 days
Result: When used in combination with Anti-PD-1, it significantly increased the infiltration of CD4+ and CD8+ T cells within tumors.
Synergistically inhibited tumor growth (reducing it by 95%) and lung metastasis.
Molecular Weight

613.79

Formula

C31H51N9O4

CAS No.
SMILES

O=C(CNCCC(N1CCC(CC1)NC2=NC(NCC3=NC(CCCNCCCNC4CCCCC4)=CO3)=NC(C)=C2)=O)O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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BPRCX807
Cat. No.:
HY-178205
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