C188-9 Chemical Properties

Boiling point:

680.9±65.0 °C(Predicted)

Density 

1.416±0.06 g/cm3(Predicted)

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

solubility 

DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml

form 

A crystalline solid

pka

8.14±0.50(Predicted)

color 

Off-white to pink

C188-9 Usage And Synthesis

Biological Activity

C188-9 (TTI 101) is a potent STAT3 inhibitor, binds STAT3 with high affinity, Kd=4.7±0.4 nM. It is well tolerated in mice, has good oral bioavailability, and is mainly enriched in tumor tissues.

in vitro

C188-9 is a small molecule inhibitor of STAT3, targeting the phosphotyrosine peptide binding site in the SH2 region of STAT3 with a Ki value of 136 nM. It does not inhibit upstream Jak or Src kinases.

in vivo

C188-9 inhibited tumor growth in mice bearing UM-SCC-17B xenografts after administration of C188-9. C188-9 was well tolerated in mice, had good oral bioavailability, and was concentrated in tumor tissue after administration.

target