Molecular Formula | C29H27F5N2O6S |
Molar Mass | 626.59 |
Density | 1.474±0.06 g/cm3(Predicted) |
Boling Point | 749.2±70.0 °C(Predicted) |
Solubility | DMSO: ≥ 33 mg/mL |
pKa | 3.15±0.10(Predicted) |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
In vitro study | BP-1-102 binds Stat3 with an affinity K D of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro , with an IC 50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8. |
In vivo study | Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.596 ml | 7.98 ml | 15.959 ml |
5 mM | 0.319 ml | 1.596 ml | 3.192 ml |
10 mM | 0.16 ml | 0.798 ml | 1.596 ml |
5 mM | 0.032 ml | 0.16 ml | 0.319 ml |
biological activity | BP-1-102 is a small molecule inhibitor of transcription factor Stat3 with oral activity, and its IC50 value is 6.8 μM. | |
target | STAT3 6.8 μM (IC 50 ) | |
in vitro study | BP-1-102 binds stat3 with an affinity K D of 504 nM. BP-1-102 inhibits stat3 DNA-binding activity in vitro , with an IC 50 value of 6.8±0.8 μ m. it blocks Stat3-phospho-tyrosine peptide interactions and stat3 activation at 4-6.8 μ m, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8. | |
in vivo research | Mick therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth. |