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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2236595-58-5
- Fòrmula: C31H51N9O4
- Peso molecular:613.79
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
CXCR4 |
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 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.
-
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).
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.
Chemical Information
-
No. CAS 2236595-58-5
-
Peso molecular 613.79
-
Fòrmula C31H51N9O4
-
SMILES
O=C(CNCCC(N1CCC(CC1)NC2=NC(NCC3=NC(CCCNCCCNC4CCCCC4)=CO3)=NC(C)=C2)=O)O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Ghasemi K, et al. MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy? Int Immunopharmacol. 2022 Jul;108:108863. [Content Brief]
[2]. Yu SJ, et al. Protective Effect of CXCR4 Antagonist CX807 in a Rat Model of Hemorrhagic Stroke. Int J Mol Sci. 2020 Sep 25;21(19):7085. [Content Brief]
[3]. Song JS, et al. A highly selective and potent CXCR4 antagonist for hepatocellular carcinoma treatment. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2015433118. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BPRCX807 Related Classifications
HY-178205 Related Classifications
Powered by Bioz