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CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. CH5138303 showed high binding affinity for N-terminal Hsp90α (Kd=0.52nM) and strong in vitro cell growth inhibition against human cancer cell lines (HCT116 IC50=0.098μM, NCI-N87 IC50=0.066μM) and also displayed high oral bioavailability in mice (F=44.0%) and potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model (tumor growth inhibition=136%).
| Cell Experiment | |
|---|---|
| Cell lines | HCT116 and NCI-N87 cell lines |
| Preparation method | Culturing HCT116 cell line and NCI-N87 cell line according to the supplier’s instructions. Suspending cells in a medium are added to solutions which contains various concentrations of the test substance, and culturing the cells at 37 °C in 5% CO2. Four days later, adding cell Counting Kit-8 solution and measuring absorbance at 450 nm with Microplate-Reader iMark. Calculating antiproliferative activity by the formula (1−T/C) × 100 (%), where T represents the absorbance of drug-treated cells and C that of untreated control cells at 450 nm. Using Microsoft Excel 2007 to calculate the 50% inhibition concentration (IC50) values |
| Concentrations | ~10 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | Mice with human NCI-N87 gastric cancer xenograft. |
| Formulation | |
| Dosages | 50 mg/kg |
| Administration | p.o. |
| Molecular Weight | 415.9 |
| Formula | C19H18ClN5O2S |
| CAS Number | 959763-06-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HSP Products |
|---|
| NCT-58
NCT-58 is a potent inhibitor of C-terminal HSP90. |
| Gedunin
Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. |
| VER-49009
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM. |
| YUM70
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity. YUM70 induces endoplasmic reticulum stress-mediated apoptosis in pancreatic cancer. |
| Hsp70-derived octapeptide
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs. |
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