[CAS NO. 432001-19-9] C188-9
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PRODUCTS SPECIFICATIONS [432001-19-9]
Store
Catalog
SLK-S8605
Brand
Selleck
CAS
432001-19-9
DESCRIPTION [432001-19-9]
Overview
| MDL | MFCD03141581 |
|---|---|
| Molecular Weight | 471.52 |
| Molecular Formula | C27H21NO5S |
| SMILES | O=S(C1=CC=C(OC)C=C1)(NC2=C3C=CC=CC3=C(O)C(C4=C5C=CC=CC5=CC=C4O)=C2)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1208 mL | 10.6040 mL | 21.2080 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2416 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL |
Description
C188-9 (TTI 101) is a potent inhibitor of that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.
Targets
| STAT3 [1] (Cell-free) |
| 4.7 nM(Kd) |
In vitro
C188-9 is a small-molecule inhibitor of Stat3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases.
In vivo
Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors.
References
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