CH5138303 is a novel and potent HSP90 inhibitor. 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%).
MedKoo Cat#: 406497
Name: CH5138303
CAS#: 959763-06-5
Chemical Formula: C19H18ClN5O2S
Exact Mass: 415.0870
Molecular Weight: 415.90
Elemental Analysis: C, 54.87; H, 4.36; Cl, 8.52; N, 16.84; O, 7.69; S, 7.71
The following data is based on the product molecular weight 415.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
