Molecular Formula | C14H9ClN2O4S2 |
Molar Mass | 368.82 |
Solubility | DMSO: 30 mg/mL (Need ultrasonic) |
Appearance | powder |
Color | white to beige |
Storage Condition | 2-8°C |
In vitro study | FX1 disrupts the formation of the BCL6 inhibitory complex, inactivates the BCL6 target gene, and mimics the phenotype of mice expressing BCL6 carrying mutations in the corepressor binding site. FX1 inhibits ABC-DLBCL cells in vitro and in vivo, and also inhibits human primary ABC-DLBCL samples in vitro. FX1 is specific for BCL6 and has a greater affinity than the natural BCL6 ligand SMRT. FX1 induced significant inhibition of BCL6 target genes in DLBCL cells, such as CASP8, CD69, CXCR4, CDKN1A and dusp5. FX1 was more potent than its predecessor generations of BCL6 inhibitors, more than 100 times more potent. More than 300 times more effective than the combination of antibiotics rifamectin and rifabutin. |
In vivo study | In mice bearing DLBCL xenografts, low doses of FX1 induced tumor regression. In SCID mice, the half-life of FX1 is about 12 hours. After FX2 treatment, the lung, intestine, heart, kidney, liver, spleen and bone marrow of specific organs were taken for H & E staining observation, no significant toxicity, inflammation and signs of infection. Peripheral blood cells from FX-1 treated mice were counted and tested for serum chemistry and the parameters were found to be normal. FX1 can cause significant inhibition of DLBCLs in DLBCL transplanted tumor mice, not only preventing the growth of the transplanted tumor, but also causing it to shrink from its original size. At concentrations as low as 25 mg/kg, the maximum effect can be achieved. The TUNEL and Ki67 staining experiments demonstrated that FX1 induced more apoptosis and growth arrest than 79-6. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.711 ml | 13.557 ml | 27.114 ml |
5 mM | 0.542 ml | 2.711 ml | 5.423 ml |
10 mM | 0.271 ml | 1.356 ml | 2.711 ml |
5 mM | 0.054 ml | 0.271 ml | 0.542 ml |
biological activity | FX1 is a selective BCL6 BTB inhibitor with an IC50 of 35 μm. Of the more than 50 kinases tested, FX1 was highly selective, and 10 μm FX1 did not significantly inhibit these kinases. FX1 can induce apoptosis. |
Target | Value |
BCL6 BTB (Cell-free assay) | 35 μM |