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CH5138303

Cat. No. M3776
CH5138303 Structure
Size Price Availability
2mg USD 170 Out of stock
5mg USD 300 Out of stock
10mg USD 510 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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%).

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 415.9
Formula C19H18ClN5O2S
CAS Number 959763-06-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors.
Suda A, et al. Bioorg Med Chem. 2014 Jan 15;22(2):892-905. PMID: 24369839.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CH5138303 supplier, HSP90, inhibitors

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