MSX-122, a partial antagonist of CXCR4, impedes the CXCR4/CXCL12 interaction with an IC50 of approximately 10 nM. It does not affect cAMP reduction mediated by the ligands CCR3/CCL5 and CCR5/CCL5. At 100 nM, MSX-122 strongly inhibits the invasion of 78% of MDA-MB-231 cells but does not affect T-tropic HIV infection or show activity in calcium flux assays[1].
体内研究
MSX-122 (10 mg/kg, i.p.) reduces inflammation caused by carrageenan and lung fibrosis from bleomycin in mice. At 4 mg/kg, i.p., daily, MSX-122 inhibits metastasis in a breast cancer metastasis animal model, and at 10 mg/kg i.p., daily, it significantly reduces hepatic micrometastases[1].
体外研究
MSX-122, a partial antagonist of CXCR4, impedes the CXCR4/CXCL12 interaction with an IC50 of approximately 10 nM. It does not affect cAMP reduction mediated by the ligands CCR3/CCL5 and CCR5/CCL5. At 100 nM, MSX-122 strongly inhibits the invasion of 78% of MDA-MB-231 cells but does not affect T-tropic HIV infection or show activity in calcium flux assays[1].
MSX-122 细胞实验
Cell Line
Concentration
Treated Time
Description
References
KYSE150 cells
100 nM
MSX-122 attenuated the HIF-1α overexpression-induced promotion of migration and invasion in KYSE150 cells
Cancer Sci. 2022 Mar;113(3):926-939
KYSE30 cells
100 nM
MSX-122 attenuated the HIF-1α overexpression-induced promotion of migration and invasion in KYSE30 cells
Cancer Sci. 2022 Mar;113(3):926-939
MSX-122 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
KYSE30-fLuc lung metastasis model
Intraperitoneal injection
10 mg/kg
Once daily for 14 consecutive days
MSX-122 inhibited the lung metastasis of KYSE30 cells
Cancer Sci. 2022 Mar;113(3):926-939
C57BL/6 mice
Radiation-induced lung fibrosis model
Intraperitoneal injection
10 mg/kg
Daily administration for 20 weeks
To evaluate the inhibitory effect of MSX-122 on radiation-induced pulmonary fibrosis. Results showed that MSX-122 significantly reduced the development of pulmonary fibrosis, while AMD3100 did not show significant suppression.
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